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Osimertinib mesylate EGFR inhibidor

Name: Osimertinib mesylate
Brand: Selleck Chemicals
SKU: S5078
Rating: 5 (109 reviews)

Cat. No.S5078

Osimertinib mesylate (AZD9291) es la forma mesilato de osimertinib, que es un fármaco inhibidor de la tirosina quinasa (TKI) oral de tercera generación del receptor del factor de crecimiento epidérmico (EGFR).

Osimertinib mesylate EGFR inhibidor Chemical Structure

Estructura química

Peso molecular: 595.71

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Control de calidad

Lote: Pureza: 99.99%

99.99

Dianas relacionadas	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Otros EGFR Inhibidores	Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) Genistein

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
PC9	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.023μM	25271963
NCI-H1975	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.024μM	25271963
Calu3	Cytotoxicity assay		72 hrs	Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.264μM	25271963
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50=15μM	25271963
PC9	Function assay		2 hrs	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50=17μM	25271963
PC9-DRH	Function assay		2 hrs	Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA, IC50=0.013μM	26756222
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA, IC50=0.015μM	26756222
HCC827	Function assay		2 hrs	Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA, IC50=0.023μM	26756222
H3255	Function assay		2 hrs	Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA, IC50=0.036μM	26756222
PC9	Function assay		2 hrs	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA, IC50=0.056μM	26756222
A549	Function assay			Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50=0.15μM	26756222
H1975	Function assay		2 hrs	Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISA, IC50=0.015μM	26968253
PC9	Function assay		2 hrs	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA, IC50=0.017μM	26968253
LoVo	Function assay		2 hrs	Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA, IC50=0.48μM	26968253
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay, IC50=0.052μM	27131639
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay, IC50=0.893μM	27131639
NCI-H1975	Function assay	1 to 1000 nM	2 hrs	Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant phosphorylation in human NCI-H1975 cells at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method	27396610
NCI-H1975	Function assay	1 to 1000 nM	2 hrs	Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method	27396610
HCC827	Function assay		3 hrs	Inhibition of EGFR E746 to A750 deletion mutant phosphorylation in human patient derived HCC827 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM	27433829
H1975	Function assay		3 hrs	Inhibition of EGFR L858R/T790M mutant phosphorylation in human patient derived H1975 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM	27433829
H3255	Function assay		3 hrs	Inhibition of EGFR L858R mutant phosphorylation in human patient derived H3255 cells incubated for 3 hrs by ELISA method, IC50=0.0041μM	27433829
HaCaT	Function assay		3 hrs	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method, IC50=0.0737μM	27433829
Sf21	Function assay			Inhibition of N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (696-end residues) expressed in baculovirus infected Sf21 insect cells, IC50=0.012μM	27996267
LoVo	Function assay		2 hrs	Inhibition of EGF-stimulated wild type EGFR phosphorylation in human LoVo cells incubated for 2 hrs followed by EGF stimulation for 10 mins by ELISA, IC50=0.48μM	27996267
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay, IC50=0.03μM	28033579
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay, IC50=1.604μM	28033579
HCC827	Function assay		96 hrs	Inhibition of EGFR delE746_A750 mutant in human HCC827 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50<0.014μM	28225269
NCI-H1975	Function assay		96 hrs	Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.019μM	28225269
A431	Function assay		96 hrs	Inhibition of wild-type EGFR in human A431 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.667μM	28225269
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM	28282122
BAF3	Function assay		72 hrs	Inhibition of full length EGFR T790M/L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM	28282122
BAF3	Function assay		72 hrs	Inhibition of full length EGFR exon 19 deletion mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM	28282122
HCC827	Function assay		72 hrs	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM	28282122
PC9	Function assay		72 hrs	Inhibition of EGFR exon 19 deletion mutant in human PC9 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.002μM	28282122
BAF3	Function assay		4 hrs	Inhibition of EGFR T790M/L858R mutant (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.002μM	28282122
NCI-H1975	Function assay		72 hrs	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.005μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.013μM	28282122
H3255	Function assay		72 hrs	Inhibition of EGFR L858R mutant in human H3255 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.033μM	28282122
BAF3	Function assay		4 hrs	Inhibition of wild-type EGFR (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.043μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.3μM	28282122
BAF3	Function assay		72 hrs	Inhibition of full length EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.31μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused INSR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.5μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.55μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused IGF1R (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.56μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM	28282122
BAF3	Growth inhibition assay		72 hrs	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50=1.2μM	28282122
NCI-H2122	Function assay		72 hrs	Inhibition of wild-type EGFR in human NCI-H2122 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=1.2μM	28282122
CHL	Growth inhibition assay		72 hrs	Growth inhibition of CHL cells after 72 hrs by CellTiter-Glo assay, GI50=2.9μM	28282122
H1355	Function assay		72 hrs	Inhibition of wild-type EGFR in human H1355 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3μM	28282122
A549	Function assay		72 hrs	Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM	28282122
H1703	Function assay		72 hrs	Inhibition of wild-type EGFR in human H1703 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM	28282122
CHO	Growth inhibition assay		72 hrs	Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay, GI50=4.2μM	28282122
NCI-H1975	Function assay	1 uM	4 hrs	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
NCI-H1975	Function assay	1 uM	4 hrs	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
HCC827	Function assay	1 uM	4 hrs	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
HCC827	Function assay	1 uM	4 hrs	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
NCI-H1975	Function assay	1 uM	48 hrs	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Function assay	1 uM	48 hrs	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Function assay	1 uM	48 hrs	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Function assay	1 uM	48 hrs	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
NCI-H1975	Function assay	1 uM	48 hrs	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Function assay	1 uM	48 hrs	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Function assay	1 uM	48 hrs	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Function assay	1 uM	48 hrs	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Antiproliferative assay			Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant, IC50=0.0616μM	28426996
NCI-H1975	Antiproliferative assay			Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant, IC50=0.067μM	28426996
HEK293	Function assay			Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis, IC50=0.57μM	28426996
A431	Antiproliferative assay			Antiproliferative activity against human A431 cells harboring wild-type EGFR, IC50=0.6156μM	28426996
Sf9	Function assay		20 mins	Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50=0.278μM	28482151
BAF3	Function assay		72 hrs	Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.006μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.016μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.018μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.02μM	28528303
BAF3	Function assay		72 hrs	Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.066μM	28528303
DFCI032	Function assay		72 hrs	Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs in presence of ceritinib by MTS assay, EC50=0.19μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=1.748μM	28528303
DFCI076	Function assay		72 hrs	Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of ceritinib, EC50=3.21μM	28528303
DFCI032	Function assay		72 hrs	Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=4.73μM	28528303
DFCI076	Function assay		72 hrs	Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=7.93μM	28528303
DFCI032	Function assay	0.1 to 1 uM		Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM by Western blot analysis	28528303
DFCI032	Function assay	0.1 to 1 uM		Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis	28528303
DFCI032	Function assay	0.1 to 1 uM		Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR mediated ERK phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis	28528303
NCI-H1975	Antiproliferative assay		96 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.019μM	28603991
A431	Antiproliferative assay		96 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.7μM	28603991
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay, IC50=0.0065μM	28716641
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay, IC50=0.0105μM	28716641
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay, IC50=0.4159μM	28716641
BEAS2B	Antiproliferative assay		72 hrs	Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay, IC50=14.9μM	28716641
HCC827	Antiproliferative assay		96 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM	28853575
NCI-H1975	Antiproliferative assay		96 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM	28853575
A431	Antiproliferative assay		96 hrs	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=0.67μM	28853575
A549	Antiproliferative assay		96 hrs	Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=1.83μM	28853575
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.019μM	29466773
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM	29466773
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=0.53μM	29466773
NCI-H1975	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.06μM	29486953
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.65μM	29486953
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50=0.87μM	29486953
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50=0.023μM	29534926
NCI-H1975	Function assay		1 hr	Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA, IC50=0.041μM	29534926
A431	Function assay		1 hr	Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA, IC50=0.141μM	29534926
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.685μM	29534926
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay, IC50=0.0254μM	29576272
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.0472μM	29576272
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.486μM	29576272
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay, IC50=0.041μM	29730192
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay, IC50=1.26μM	29730192
NCI-H1975	Antitumor assay	10 mg/kg	21 days	Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days	29730192
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.019μM	29853340
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM	29853340
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=0.53μM	29853340
NCI-H1975	Function assay	1 to 100 nM		Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method	29906114
NCI-H1975	Function assay	100 nM		Inhibition of EGFR L858R/T790M double mutant in EGF-stimulated human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Ser-473 residue at 100 nM by Western blot method	29906114
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells preincubated for 2 hrs followed by compound washout measured up to 24 hrs by Western blot method	29906114
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in ERK1/2 phosphorylation preincubated for 2 hrs followed by compound washout measured after 12 hrs by Western blot method	29906114
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay, IC50=0.13μM	30429956
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay, IC50=1.24μM	30429956
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=4.61μM	30429956
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=5.15μM	30429956
BAF3	Function assay	1 to 3 uM	2 hrs	Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
BAF3	Function assay	1 to 3 uM	2 hrs	Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, GI50=0.0028μM	30442506
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.011μM	30442506
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, GI50=0.0401μM	30442506
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, IC50=0.06μM	30442506
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.16μM	30442506
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.61μM	30442506
Calu3	Antiproliferative assay		72 hrs	Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.75μM	30442506
Calu6	Antiproliferative assay		72 hrs	Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=5.86μM	30442506
NCI-H1975	Function assay		4 hrs	Inhibition of EGFR T790M/L858R double mutant phosphorylation at Y1068 residue in human NCI-H1975 cells up to 10 uM after 4 hrs by Western blot analysis	30442506
NCI-H1975	Function assay	up to 10 uM	4 hrs	Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis	30442506
A431	Function assay		4 hrs	Inhibition of WT EGFR phosphorylation at Y1068 residue in human A431 cells up to 10 uM after 4 hrs by Western blot analysis	30442506
A431	Function assay	up to 10 uM	4 hrs	Inhibition of WT EGFR in human A431 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis	30442506
Sf9	Function assay		60 mins	Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.0208μM	30471829
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay, IC50=0.096μM	30471829
Sf9	Function assay		60 mins	Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.5675μM	30471829
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.945μM	30471829
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3.242μM	30471829
Aspc-1	Antiproliferative assay		72 hrs	Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay, IC50=3.985μM	30471829
NCI-H1975	Growth inhibition assay		72 hrs	Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.1μM	30472599
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.073μM	30530173
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.615μM	30530173
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50=1.605μM	30530173
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay, IC50=0.03μM	31223440
A431	Antiproliferative assay		72 hrs	Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay, IC50=1.44μM	31223440
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay, IC50=3.93μM	31223440
BAF3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay, IC50=5.11μM	31223440
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50<0.01μM	31446247
CL68	Antiproliferative assay		72 hrs	Antiproliferative activity against human CL68 cells harbouring EGFR delE746-A750/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.01μM	31446247
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.05μM	31446247
CL97	Antiproliferative assay		72 hrs	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.1μM	31446247
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5μM	31446247
A431	Cytotoxicity assay		96 hrs	Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method, CC50=0.967μM	31560541
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.014μM	31581004
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.016μM	31581004
NCI-H292	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.084μM	31581004
LO2	Cytotoxicity assay		72 hrs	Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.602μM	31581004
HEK293A	Cytotoxicity assay		72 hrs	Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=2.418μM	31581004
HK2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=3.565μM	31581004
HLF	Cytotoxicity assay		72 hrs	Cytotoxicity against human HLF cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=8.741μM	31581004
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.073μM	31683104
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.462μM	31683104
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.975μM	31683104
HeLa	Function assay	0.1 to 5 uM	24 hrs	Inhibition of EFGR protein expression in human HeLa cells at 0.1 to 5 uM after 24 hrs by Western blot analysis	31683104
BAF3	Function assay		72 hrs	Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.001μM	31689114
BAF3	Function assay		72 hrs	Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.081μM	31689114
A431	Antiproliferative assay		96 hrs	Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.084μM	31689114
BAF3	Function assay		72 hrs	Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.78μM	31689114
BAF3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=1.1μM	31689114
BaF3	Function assay		4 hrs	Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay, IC50=3.1μM	31689114
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay, IC50=0.07μM	31718182
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay, IC50=3.1μM	31718182
NCI-H1975	Cytotoxicity assay		4 days	Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.013μM	ChEMBL
A549	Cytotoxicity assay		4 days	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.31μM	ChEMBL
Vero	Antiviral assay		24 hrs	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50=3.26μM	ChEMBL
Vero	Cell viability assay		72hrs	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr, CC50=13.23μM	ChEMBL
NCI-H1975	Function assay		16 hrs	Inhibition of EGFR T790M/L858R double mutant phosphorylation in human NCI-H1975 cells up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis	ChEMBL
NCI-H1975	Function assay		16 hrs	Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as AKT phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis	ChEMBL
NCI-H1975	Function assay		16 hrs	Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as ERK1/2 phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis	ChEMBL
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Información química, almacenamiento y estabilidad

Peso molecular	595.71	Fórmula	C₂₉H₃₇N₇O₅S	Almacenamiento (Desde la fecha de recepción)	3 years -20°C powder
Nº CAS	1421373-66-1	--		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	AZD9291 mesylate			Smiles	CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC.CS(=O)(=O)O

Solubilidad

In vitro
Lote:

DMSO : 5 mg/mL (8.39 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL (33.57 mM) Calentado con baño de agua a 50°C; Ultrasonido;
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.250mg/ml (2.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	0.625mg/ml (1.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC₅₀/Ki	EGFR
In vitro	Las células de adenocarcinoma de pulmón (LUAD) resistentes a Osimertinib expresan un nivel más alto de METTL7B en comparación con las células sensibles a Osimertinib. La reducción de METTL7B mediante GNC-siRNA resensibilizó las células LUAD a osimertinib.
In vivo	El METTL7B se incrementa significativamente tanto a nivel de ARNm como de proteínas en los xenoinjertos resistentes a osimertinib en comparación con los xenoinjertos sensibles a osimertinib. En el modelo de ratón LUAD CDX, el tratamiento combinado con GNC-siMETTL7B (6 mg de siRNA por equivalente de ratón) suprime significativamente el crecimiento tumoral en comparación con el tratamiento de osimertinib (30 mg/kg) solo.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/35144642/ [2] https://pubmed.ncbi.nlm.nih.gov/31564718/

Soporte técnico

Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

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