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LY294002 PI3K inhibidor

Name: LY294002
Brand: Selleck Chemicals
SKU: S1105
Rating: 5 (1657 reviews)

Cat. No.S1105

LY294002 (SF 1101, NSC 697286) es la primera molécula sintética conocida por inhibir PI3Kα/δ/β con IC50 de 0,5 μM/0,57 μM/0,97 μM, respectivamente; más estable en solución que la Wortmannina, y también bloquea la formación de autofagosomas. No solo se une a las PI3K de clase I y a otras quinasas relacionadas con PI3K, sino también a nuevos objetivos aparentemente no relacionados con la familia PI3K. Este compuesto también inhibe CK2 con una IC50 de 98 nM. Es un inhibidor no específico de DNA-PKcs y activa la autophagy y la apoptosis.

LY294002 PI3K inhibidor Chemical Structure

Estructura química

Peso molecular: 307.34

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Control de calidad

Lote: Pureza: 99.99%

99.99

Dianas relacionadas	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Otros PI3K Inhibidores	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549) Paxalisib (GDC-0084)

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
Sf9 cells	Function assay			Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM.	10998351
HeLa cells	Binding affinity assay			Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM	15658870
HeLa cells	Function assay			Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM.	15658870
HeLa (human carcinoma) cells.	Function assay			In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM.	15658870
human PC3 cells	Proliferation assay	25 μM	120 h	Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO	16680159
human BJ cells	Function assay	25 μM	2 h	Activation of Akt phosphorylation at Thr308 in PDGF-stimulated serum starved human BJ cells at 25 uM treated 2 hrs before PDGF challenge by immunoblotting	16767085
human BJ cells	Function assay	25 μM	2 h	Inhibition of PI3K signaling in PDGF-stimulated serum starved human BJ cells transfected with plasmid EGFP/PH domain of Akt assessed as suppression of PH-EGFP redistribution to plasma membrane at 25 uM treated 2 hrs before PDGF challenge by confocal microscopy	16767085
mouse mast cells	Function assay	20 μM		Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM	16789742
THP1 cells	Function assay			Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM.	16789742
mouse Raw264 macrophage	Function assay			Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM.	16789742
THP1 cells	Function assay			Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM.	16789742
THP1 cells	Function assay			Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM.	16789742
human A375 cells	Proliferation assay		46 h	Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM.	17049248
HeLa cells	Function assay			Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM.	17135248
human SW480 cells	Function assay	20 μM	24 h	Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis	17472962
human A375 cells	Proliferation assay			Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM.	17601739
human A2780 cells	Apoptosis assay	2 μM	12 h	Induction of apoptosis in cisplatin-resistant human A2780 cells assessed as decrease in phosphorylated Akt level at 2 uM after 12 hrs by immunoblot analysis.	17684018
human H4 cells	Function assay		2 h	Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control	18024584
Sf9 cells	Function assay			Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM.	18321716
rat RBL2H3 cells	Function assay			Inhibition of A23187-induced degranulation in rat RBL2H3 cells	18328716
human U87MG cells	Function assay			Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM.	18345609
human H460 cells	Function assay	30 μM		Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM	18501601
human U251HRE cells	Function assay			Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay	18501601
human 184B5 cells	Cytotoxic assay			Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM.	18691894
human MDA-MB-468 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM.	18691894
human MDA-MB-468 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=8.2 μM.	18691894
MDA-MB-231 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM.	18691894
human MDA-MB-468 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay， IC50=4.76 μM.	18691894
human MDA-MB-231 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.35 μM.	18691894
human MDA-MB-231 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-231 cells in presence of 20 μM chloroquine by SRB assay, GI=3.32 μM.	18691894
human MCF7 cells	Cytotoxic assay			Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 μM.	18691894
human MCF7 cells	Cytotoxic assay			Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=3.08 μM.	18691894
human MCF7 cells	Cytotoxic assay			Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM.	18691894
Sf21 cells	Function assay			Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM.	19748269
Sf9 cells	fluorescent polarization assay			Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay	21121631
Sf9 cells	Fluorescent polarization assay			Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM.	21121631
human IGROV1 cells	Function assay		24 h	Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 5 fold IC50 after 24 hrs by flow cytometry	21216151
human IGROV1 cells	Function assay		24 h	Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 1 fold IC50 after 24 hrs by flow cytometry	21216151
human IGROV1 cells	Function assay		24/48 h	Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in cyclin D1 level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis	21216151
human IGROV1 cells	Function assay		24/48 h	Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in phosphorylated AKT level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis	21216151
human HCT116 cells	Cytotoxic assay		72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM.	21945250
human KB cells	Cytotoxic assay		72 h	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM.	21945250
HUVEC	Function assay	10-25 μM	30 min	Inhibition of TNFalpha-stimulated human ICAM-1 promoter activity expressed in HUVEC assessed as beta-galactosidase activity at 10 to 25 uM pretreated for 30 mins before TNFalpha challenge measured after 5 hrs by luciferase reporter gene assay	22026410
HUVEC	Function assay	10-25 μM	16 h	Inhibition of TNFalpha-stimulated ICAM-1 mRNA expression in HUVEC at 10 to 25 uM pretreated for 16 hrs before TNFalpha challenge measured after 6 hrs by RT-PCR analysis	22026410
human HCT116 cells	Function assay	10 μM		Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis	22212721
human HCT116 cells	Function assay	10 μM		Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis	22212721
human HCT116 cells	Function assay	10 μM		Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis	22212721
human HCT116 cells	Function assay	10 μM	10 min	Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	22212721
human HCT116 cells	Function assay	10 μM	10 min	Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	22212721
human HCT116 cells	Growth inhibition assay		48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=6.7 μM.	22212721
human HCT116 cells	Growth inhibition assay		48 h	Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=5.8 μM.	22212721
human HCT116 cells	Growth inhibition assay		48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM	22212721
human A549 cells	Cytotoxic assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	22480851
human PC3 cells	Cytotoxic assay		72 h	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM.	22480851
human HL60 cells	Cytotoxic assay		72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM.	22480851
Sf21 cells	Function assay			Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50=0.5 μM	22520630
HEK293 cells	Function assay		1.5 h	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	22537153
human H1299 cells	Function assay	0.1-30 μM	24 h	Induction of JNK-mediated CHOP expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H1299 cells	Function assay	0.1-30 μM	24 h	Induction of DR5 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H1299 cells	Function assay	0.1-30 μM	24 h	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis in presence of 100 ug/ml TRAIL and PI3K inhibitor LY294002	22622069
human H1299 cells	Function assay	0.1-30 μM	24 h	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
MDA-MB-231 cells	Cell invasion assay		24 h	Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay, IC50=0.38 μM.	22804108
human LNCAP cells	Function assay	0.1-30 μM	24 h	Downregulation of survivin expression in human LNCAP cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22832316
human LNCAP cells	Function assay	0.1-30 μM	30 min	Inhibition of Akt phosphorylation in human LNCAP cells at 0.1 to 30 uM after 30 mins by Western blot analysis	22832316
human PC3 cells	Function assay	50 μM	8 h	Induction of p21 protein expression in human PC3 cells at 50 uM incubated for 8 hrs by Western blotting relative to untreated control	22998472
human BT474 cell	Proliferation assay		72 h	Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis， IC50=20.7 μM.	23410005
human PC3 cell	Proliferation assay		72 h	Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=12.1 μM.	23410005
human PC3 cells	Function assay		30 min	Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA, IC50=1.3μM.	23410005
human MGC803 cells	Function assay	25 μM	48 h	Cell cycle arrest in human MGC803 cells assessed as accumulation at G2/M phase at 25 uM after 48 hrs using propidium iodide staining after 48 hrs by flow cytometer relative to control	24119869
mouse RAW264.7 cells	Function assay	25 μM	20 h	Inhibition of PI3K/AKT in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS protein expression at 25 μM after 20 hrs by Western blot analysis	24299616
human A549 cells	Proliferation assay		72 h	Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=82.32 μM.	25693787
human HuH7 cells	Proliferation assay		72 h	Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=67.18 μM.	25693787
human HCT116 cells	Proliferation assay		72 h	Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=51.82 μM.	25693787
human HL60 cells	Proliferation assay		72 h	Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=18.43 μM.	25693787
Sf9 cells	Function assay			Inhibition of His-tagged human CK2 expressed in Sf9 cells, IC50 = 6.9 μM.	10998351
HeLa cells	Function assay			In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells., IC50 = 1.4 μM.	12941339
HeLa cells	Function assay			Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50 = 1.5 μM.	15658870
Sf21 cells	Function assay			Inhibition of human recombinant PI3Kbeta expressed in baculovirus-infected Sf21 cells, IC50 = 0.9 μM.	19748269
Sf21 cells	Function assay			Inhibition of bovine recombinant PI3Kgamma expressed in baculovirus-infected Sf21 cells, IC50 = 7 μM.	19748269
HeLa cells	Function assay			Activity at PI3K in human HeLa cells by ELISA, EC50 = 1.5 μM.	20092323
Sf21 cells	Function assay			Inhibition of PI3Kdelta expressed in cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.57 μM.	22520630
Sf21 cells	Function assay			Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.97 μM.	22520630
HL60 cells	Antiproliferative assay		3 days	Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay, IC50 = 14 μM.	26945110
U937 cells	Antiproliferative assay		3 days	Antiproliferative activity against human U937 cells measured after 3 days by MTS assay, IC50 = 14 μM.	26945110
Jurkat cells	Antiproliferative assay		3 days	Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay, IC50 = 22 μM.	26945110
K562 cells	Antiproliferative assay		3 days	Antiproliferative activity against human K562 cells measured after 3 days by MTS assay, IC50 = 38 μM.	26945110
U266 cells	Antiproliferative assay		3 days	Antiproliferative activity against human U266 cells measured after 3 days by MTS assay, IC50 = 46 μM.	26945110
MDA-MB-231 cells	Antimigratory assay		24 hrs	Antimigratory activity against EGF induced chemotaxis in human MDA-MB-231 cells preincubated for 24 hrs followed by EGF addition for 3.5 hrs by light microscopy, IC50 = 0.38 μM.	27598237
MDA-MB-231 cells	Antiinvasive assay		3.5 hrs	Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs, IC50 = 0.38 μM.	28009521
HEK293T cells	Function assay		1 hr	Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 0.42 μM.	28280261
HEK293T cells	Function assay		1 hr	Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 1.53 μM.	28280261
HEK293T cells	Function assay		1 hr	Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 2.37 μM.	28280261
MDA-MB-231 cells	Function assay			Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay, IC50 = 0.38 μM.	28302401
MCF7 cells	Function assay	10 uM	1 hr	Inhibition of IGF1R phosphorylation at Tyr1161 residue in human MCF7 cells at 10 uM after 1 hr by Hoechst 33258 staining based immunohistochemical analysis	28557430
SKOV3 cells	Function assay	20 uM	24 hrs	Inhibition of BDNF-induced invasion in human SKOV3 cells at 20 uM after 24 hrs in by matrigel invasion assay	29122484
SKOV3 cells	Antimigratory assay	20 uM	24 hrs	Antimigratory activity against human SKOV3 cells assessed as inhibition of BDNF-induced cell migration at 20 uM after 24 hrs by scratch wound healing assay	29122484
NB1643 cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50 cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2 cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
J774 cells	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA, IC50 = 3.7 μM.	29726680
J774 cells	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA, IC50 = 5.1 μM.	29726680
J774 cells	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 8.9 μM.	29726680
J774 cells	Function assay	10 uM	4 hrs	Inhibition of PI3K/Akt in mouse J774 cells assessed as reduction in LPS-induced Akt phosphorylation at Ser473 at 10 uM after 4 hrs by Western blot analysis	29726680
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Información química, almacenamiento y estabilidad

Peso molecular	307.34	Fórmula	C₁₉H₁₇NO₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	154447-36-6	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	SF 1101, NSC 697286			Smiles	C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4

Solubilidad

In vitro
Lote:

DMSO : 80 mg/mL (260.29 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 15 mg/mL

Water : 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.
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.	3.400mg/ml (11.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 68 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.
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%absolute ethyl alcohol 1 95%Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.000mg/ml (3.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear absolute ethyl alcohol 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.
Clear solution	5%DMSO 1 20%PEG300 2 5%Tween80 3 70%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	3.500mg/ml (11.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 200 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 700 μL of ddH2O to adjust the volume to 1 mL. 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.
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.	3.000mg/ml (9.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 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 make it clear; 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.

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	CK2 (Cell-free assay) 98 nM p110α (Cell-free assay) 0.5 μM p110δ (Cell-free assay) 0.57 μM p110β (Cell-free assay) 0.97 μM DNA-PK (Cell-free) 1.4 μM
In vitro	LY294002 no es exclusivamente selectivo para las PI3K, y de hecho podría actuar sobre otras quinasas lipídicas y proteínas adicionales aparentemente no relacionadas. Se ha demostrado que este compuesto inhibe no solo mTOR y DNA-PK, sino también otras proteínas quinasas, como CK2 (casein kinase 2) y Pim-1. Inactiva Akt/PKB, lo que consecuentemente inhibe la proliferación celular e induce la apoptosis. Este químico demuestra un notable efecto inhibitorio del crecimiento e inductor de apoptosis en estas líneas celulares de cáncer de colon, con una disminución de la expresión de Akt fosforilado (Ser473). Induce una marcada picnosis nuclear y un volumen citoplasmático disminuido en las células tumorales. Así, este compuesto inhibe marcadamente la proliferación de células de cáncer de ovario in vitro. Induce una detención específica de G1 en el crecimiento celular, lo que lleva a una inhibición casi completa de la proliferación de células de melanoma y una inhibición parcial de la proliferación de MG-63 (línea celular de osteosarcoma). El efecto de este químico en la progresión del ciclo celular puede proporcionar información sobre un posible vínculo entre la vía de activación de PI3K y la regulación del ciclo celular del cáncer.
Ensayo de quinasa	ensayos de quinasas
Ensayo de quinasa	La inhibición de PI3K por LY294002 se determina en un ensayo radiométrico utilizando enzimas purificadas y recombinantes con 1 μM de ATP. La reacción de quinasa se lleva a cabo durante 1 hora a temperatura ambiente (24°C) y se termina con la adición de PBS. Los valores de IC50 se determinan posteriormente utilizando un ajuste de curva dosis-respuesta sigmoidal (pendiente variable). La inhibición de CK2 y GSK3β (glycogen synthase kinase 3β) se establece mediante un cribado de selectividad de quinasas. Este compuesto se prueba contra el panel de quinasas de Upstate en 10 μM de ATP.
In vivo	LY294002 también produce la supresión del crecimiento tumoral y la inducción de apoptosis, especialmente en los tumores LoVo, y por lo tanto muestra una eficacia notable en el modelo murino de carcinomatosis peritoneal. Este compuesto inhibe significativamente el crecimiento y la formación de ascitis del carcinoma ovárico.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/17362206/ [2] https://pubmed.ncbi.nlm.nih.gov/12060641/ [3] https://pubmed.ncbi.nlm.nih.gov/10741711/ [4] https://pubmed.ncbi.nlm.nih.gov/17302559/ [5] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1868829/ [6] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3560216/

Aplicaciones

Métodos	Biomarcadores	PMID
Western blot	E-cadherin / p-Akt / Akt beta-catenin / p-GSK3β / Cyclin D1 Bcl-xl / Bax / caspase3 / cleaved caspase-3 p-p70S6K (T389) / p-GSK3β(S9) / pERK / Vinculin pPKB-S473	29731993
Growth inhibition assay	Cell viability	25344912
Immunofluorescence	α-SMA / CD31 E-cadherin / beta-catenin COX-2 / p-NFκB FOXO3a	27671604
ELISA	IL-10 / IL-1β / TNFα / IL-6	22208359

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT02337309	Terminated	Neuroblastoma	New Approaches to Neuroblastoma Therapy Consortium\|SignalRX Pharmaceuticals Inc.\|University of Southern California	July 9 2015	Phase 1

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Preguntas frecuentes

Pregunta 1:
I want to buy a inhibitor that can inactivates Akt/PI3K. I notice the protocol of this compound (catalog no. s1105) says it will inactivates Akt/PKB. Is it available for Akt/PI3K inhibition?

Respuesta:
It is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively. This compound can inhibit PI3K/AKT. PKB is the alternative name of AKT.

Pregunta 2:
What is the suggested formulation of this compound for mouse injection(i.p.)?

Respuesta:
It can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly, and the concentration of DMSO is safe for in vivo experiments.

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