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Daunorubicin Hydrochloride (Daunomycin) Inhibidor de la Topoisomerase II

Name: Daunorubicin Hydrochloride (Daunomycin)
Brand: Selleck Chemicals
SKU: S3035
Rating: 5 (80 reviews)

Cat. No.S3035

Daunorubicin HCl inhibe tanto la síntesis de DNA como de RNA e inhibe la síntesis de DNA con un K_i de 0,02 μM en un ensayo libre de células. Daunorubicin es un inhibidor de la topoisomerase II que induce la apoptosis.El Daunorubicin (RP 13057) HCl puede utilizarse para inducir modelos animales de enfermedad renal.

Daunorubicin Hydrochloride (Daunomycin) Topoisomerase inhibidor Chemical Structure

Estructura química

Peso molecular: 563.98

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Control de calidad

Lote: Pureza: 99.98%

99.98

Dianas relacionadas	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Otros Topoisomerase Inhibidores	Camptothecin (CPT) Betulinic acid Beta-Lapachone (S)-10-Hydroxycamptothecin Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Cu(II)-Elesclomol Hydroxy Camptothecine Rubitecan

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
MDA MB 361(mammary carcinoma cell line)	Cytotoxic assay			The compound was tested for intracellular cytotoxicity against MDA MB 361(mammary carcinoma cell line) expressing LacZ (beta-galactosidase), IC50=17 nM	10395490
P388 leukemia cell line	Cytotoxic assay			Compound was evaluated for cytotoxicity against P388 leukemia cell line, IC50=3 nM	10479297
Dx5 w/PSC cell lines	Growth inhibition assay			The compound was evaluated for the growth inhibition of Dx5 w/PSC cell lines using MTT assay, IC50=14 nM	10698449
MES-SA uterine tumor cell lines	Growth inhibition assay			The compound was evaluated for the growth inhibition of MES-SA uterine tumor cell lines using MTT assay, IC50=0.021 μM	10698449
Dx5 cell lines	Growth inhibition assay			The compound was evaluated for the growth inhibition of Dx5 cell lines using MTT assay, ic50=2 μM	10698449
human epidermoid carcinoma cell line KB-3-1	Cytotoxic assay			In vitro cytotoxic activity was evaluated using the human epidermoid carcinoma cell line KB-3-1, IC50=7 nM	12443763
human uterine sarcoma cell line MES-SA	Cytotoxic assay			In vitro cytotoxic activity was evaluated using the human uterine sarcoma cell line MES-SA, IC50=0.07 μM	12443763
Jurkat T lymphocytes	Cytotoxic assay			Cytotoxicity against Jurkat T lymphocytes by MTT assay, IC50=0.0826 μM	16366602
human HeLa3 cell line	Cytotoxic assay			Cytotoxicity against human HeLa3 cell line by MTT assay, IC50=2.96 μM	16942037
NCI-H69 cell line	Proliferation assay			Antiproliferative activity against drug sensitive NCI-H69 cell line by Alamar Blue assay, IC50=0.1 μM	17286393
L1210	Function assay			Inhibition of RNA synthesis in mouse L1210 cells, ED50 = 0.3 μM.	423181
L1210	Function assay			Inhibition of DNA synthesis in mouse L1210 cells, ED50 = 1 μM.	423181
L1210	Function assay			Inhibition of RNA synthesis in mouse L1210 cells assessed as inhibition of [3H]uridine incorporation, ED50 = 0.3 μM.	490537
L1210	Function assay			Inhibition of DNA synthesis in mouse L1210 cells assessed as inhibition of [3H]thymidine incorporation, ED50 = 0.4 μM.	490537
L1210	Function assay			Inhibition of [3H]uridine incorporation into proliferating L1210 cells, ED50 = 0.33 μM.	6716401
L1210	Function assay			Inhibition of [3H]thymidine incorporation into proliferating L1210 cells, ED50 = 0.66 μM.	6716401
L1210	Function assay			Dose required to inhibit the RNA synthesis in leukemia L1210 cells, ED50 = 0.3 μM.	7252976
L1210	Function assay			Dose required to inhibit the DNA synthesis in leukemia L1210 cells, ED50 = 1 μM.	7252976
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.22 μM.	17190447
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.25 μM.	17190447
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.32 μM.	17190447
PC-3	Cytotoxicity assay		48 hrs	Cytotoxicity against human PC-3 cells after 48 hrs by MTT assay, IC50 = 0.44 μM.	17190447
Yoshida sarcoma tumor cells	Function assay			Concentration inhibiting [3H]TdR incorporation in Yoshida sarcoma tumor cells in vitro in rats, IC50 = 0.02 μM.	1322986
HL60	Apoptosis assay			In vitro concentration required to induce apoptosis in HL60 cells, AC50 = 0.04 μM.	12877593
HL60R	Apoptosis assay			In vitro concentration required to induce apoptosis in HL60R cells, AC50 = 10 μM.	12877593
HL60	Cytotoxicity assay			Cytotoxicity against human HL60 cells after 48 hrs by trypan blue exclusion method, AC50 = 0.1 μM.	18339455
HL60	Apoptosis assay			Induction of apoptosis in multidrug resistant human HL60 cells after 48 hrs, AC50 = 38 μM.	18339455
HTB-81	Cytotoxicity assay			Cytotoxicity that caused a 50% reduction in absorbance at 490 nm in human prostate cancer HTB-81 cells using MTS assay, EC50 = 0.058 μM.	11020285
B16	Cytotoxicity assay			Cytotoxicity that caused a 50% reduction in absorbance at 490 nm in B16 mouse melanoma cells using MTS assay, EC50 = 0.16 μM.	11020285
fibroblast (NHF) cells	Cytotoxicity assay			Cytotoxicity that caused a 50% reduction in absorbance at 490 nm in normal human fibroblast (NHF) cells using MTS assay, EC50 = 0.22 μM.	11020285
L1210	Function assay		3 hrs	Inhibition of DNA synthesis in mouse L1210 cells preincubated for 3 hrs followed by [3H]-thymidine addition measured after 1 hr by scintillation spectrometric analysis, ED50 = 0.3 μM.	176359
L1210	Function assay		3 hrs	Inhibition of RNA synthesis in mouse L1210 cells preincubated for 3 hrs followed by [3H]-uridine addition measured after 1 hr by scintillation spectrometric analysis, ED50 = 0.3 μM.	176359
L1210	Function assay			Inhibition of RNA synthesis in mouse L1210 cells, ED50 = 0.33 μM.	423182
L1210	Function assay			Inhibition of DNA synthesis in mouse L1210 cells, ED50 = 0.66 μM.	423182
L1210	Function assay			Inhibition of RNA synthesis in mouse L1210 cells, ED50 = 0.33 μM.	490536
L1210	Function assay			Inhibition of DNA synthesis in mouse L1210 cells, ED50 = 0.66 μM.	490536
L1210	Function assay			Inhibition of RNA synthesis in mouse L1210 cells, ED50 = 0.23 μM.	690999
L1210	Function assay			Inhibition of DNA synthesis in mouse L1210 cells, ED50 = 0.48 μM.	690999
L1210	Function assay			Compound was evaluated for the 50% inhibition of the incorporation of [3H]- thymidine in the RNA (inhibition of synthesis in leukemia L1210 cells), ED50 = 0.33 μM.	3761325
L1210	Function assay			Compound was evaluated for the 50% inhibition of the incorporation of [3H]- thymidine in the DNA (inhibition of synthesis in leukemia L1210 cells), ED50 = 0.66 μM.	3761325
L1210	Function assay			Concentration of drug necessary to reduce by 50% the incorporation of tritiated uridine in the RNA of actively growing L1210 cells, ED50 = 0.33 μM.	7086816
L1210	Function assay			Concentration of drug necessary to reduce by 50% the incorporation of tritiated thymidine in the DNA of actively growing L1210 cells, ED50 = 0.66 μM.	7086816
NCI60	Growth inhibition assay			Growth inhibition of human NCI60 cells, GI50 = 0.044 μM.	19944612
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay, GI50 = 0.02 μM.	19968258
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by sulforhodamine B assay, GI50 = 0.07 μM.	19968258
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, GI50 = 0.08 μM.	19968258
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by XTT assay, GI50 = 0.0074 μM.	20591678
NCI-H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H460 cells after 72 hrs by XTT assay, GI50 = 0.38 μM.	20591678
SF268	Cytotoxicity assay		72 hrs	Cytotoxicity against human SF268 cells after 72 hrs by XTT assay, GI50 = 0.6 μM.	20591678
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay, GI50 = 0.86 μM.	20591678
Detroit 551	Cytotoxicity assay		72 hrs	Cytotoxicity against human Detroit 551 cells after 72 hrs by XTT assay, GI50 = 1.77 μM.	20591678
HL60	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60 cells assessed as growth inhibition after 48 hrs by trypan blue staining-based hemocytometric analysis, GI50 = 0.1 μM.	25874335
HL60R	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60R cells expressing p-glycoprotein assessed as growth inhibition after 48 hrs by trypan blue staining-based hemocytometric analysis, GI50 = 38 μM.	25874335
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay, IC50 = 0.028 μM.	2778449
HT-29	Antiproliferative assay		96 hrs	Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay, IC50 = 0.133 μM.	2778449
HeLa	Function assay			TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.05 uM) in membrane vesicle from MRP1-expressing HeLa cells, IC50 = 8 μM.	8621644
breast carcinoma line cells	Function assay			compound was tested in vitro for inhibition activity against a sensitive human breast carcinoma line cells, IC50 = 0.06 μM.	9258351
breast carcinoma line cells	Function assay			compound was tested in vitro for inhibition activity against doxorubicin resistant counterpart of human breast carcinoma line cells, IC50 = 2 μM.	9258351
MCF-7	Function assay			Compound was tested for its toxicity against human breast cancer cells(MCF-7), IC50 = 0.06 μM.	9548820
MCF-7/ADR	Function assay			Compound was tested for its toxicity against doxorubicin resistant human breast cancer cells (MCF-7/ADR), IC50 = 2 μM.	9548820
L1210	Function assay			Inhibitory activity was measured against murine L1210 leukemia cells, IC50 = 0.03 μM.	9733483
HL60	Function assay			In vitro inhibitory concentration against proliferation of HL60 cells, IC50 = 0.005 μM.	12877593
HL60R	Function assay			In vitro inhibitory concentration against proliferation of HL60R cells along with 5 (uM) verapamil, IC50 = 0.04 μM.	12877593
HL60R	Function assay			In vitro inhibitory concentration against proliferation of HL60R cells, IC50 = 1.5 μM.	12877593
K562	Cytotoxicity assay			Cytotoxicity against K562 cells by MTS, IC50 = 0.015 μM.	16451059
P388	Antiproliferative assay			Antiproliferative activity against P388 cells by ELISA, IC50 = 0.025 μM.	17154505
P388	Antiproliferative assay			Antiproliferative activity against adriamycin resistant P388 cells in presence of 5 uM verapamil by ELISA, IC50 = 0.04 μM.	17154505
MDA435/LCC6	Antiproliferative assay			Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50 = 0.079 μM.	17154505
P388	Antiproliferative assay			Antiproliferative activity against adriamycin resistant P388 cells in presence of 5 uM 1,13-bis[4'-((5,7-dihydroxy)-4H-chromen-4-on-2-yl)phenyl]-1,4,7,10,13-pentaoxatridecane by ELISA, IC50 = 0.106 μM.	17154505
MDA435/LCC6	Antiproliferative assay			Antiproliferative activity against multidrug resistant MDA435/LCC6 cells in presence of 5 uM 1,13-bis[4'-((5,7-dihydroxy)-4H-chromen-4-on-2-yl)phenyl]-1,4,7,10,13-pentaoxatridecane by ELISA, IC50 = 0.129 μM.	17154505
MDA435/LCC6	Antiproliferative assay			Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA, IC50 = 0.977 μM.	17154505
P388	Antiproliferative assay			Antiproliferative activity against adriamycin resistant P388 cells by ELISA, IC50 = 2.111 μM.	17154505
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50 = 0.11749 μM.	17890094
A2780/ADR	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780/ADR cells after 72 hrs by MTT assay, IC50 = 18.6209 μM.	17890094
NIH/3T3	Cytotoxicity assay		72 hrs	Intrinsic cytotoxicity against wild type mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50 = 0.044 μM.	18954040
NIH/3T3	Cytotoxicity assay		72 hrs	Intrinsic cytotoxicity against mouse NIH/3T3 cells overexpressing MDR1 after 72 hrs by MTT assay, IC50 = 1.01 μM.	18954040
KB	Cytotoxicity assay		48 hrs	Cytotoxicity against human KB cells after 48 hrs by MTT assay, IC50 = 0.64 μM.	20363142
KB-C2	Cytotoxicity assay		48 hrs	Cytotoxicity against human multidrug-resistant KB-C2 cells after 48 hrs by MTT assay, IC50 = 16.2 μM.	20363142
HT-29	Cytotoxicity assay		24 hrs	Cytotoxicity against human HT-29 cells after 24 hrs by MTS assay, IC50 = 0.4 μM.	21094049
HepG2	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay, IC50 = 0.7 μM.	21094049
NIH/3T3	Cytotoxicity assay		3 days	Cytotoxicity against mouse NIH/3T3 cells after 3 days by MTS assay, IC50 = 1.8 μM.	21094049
Vero	Cytotoxicity assay		3 days	Cytotoxicity against african green monkey Vero cells after 3 days by MTS assay, IC50 = 2.5 μM.	21094049
MCF7	Cytotoxicity assay		24 hrs	Cytotoxicity against human MCF7 cells after 24 hrs by MTS assay, IC50 = 5.5 μM.	21094049
CRL7761	Cytotoxicity assay		3 days	Cytotoxicity against human CRL7761 cells after 3 days by MTS assay, IC50 = 10.5 μM.	21094049
NCI-H460	Anticancer assay			Anticancer activity against human NCI-H460 cells, IC50 = 0.38 μM.	21599000
SF268	Anticancer assay			Anticancer activity against human SF268 cells, IC50 = 0.6 μM.	21599000
MRC5	Antiproliferative assay			Antiproliferative activity against human MRC5 cells, IC50 = 0.88 μM.	21599000
MCF7	Anticancer assay			Anticancer activity against human MCF7 cells, IC50 = 5.03 μM.	21599000
DU145	Antiproliferative assay		72 hrs	Antiproliferative activity against human DU145 cells after 72 hrs by MTS assay, IC50 = 0.09 μM.	22260166
SKMES1	Antiproliferative assay		72 hrs	Antiproliferative activity against human SKMES1 cells after 72 hrs by MTS assay, IC50 = 0.17 μM.	22260166
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 0.95 μM.	22260166
LNCAP	Cytostatic assay		4 days	Cytostatic activity against human LNCAP cells after 4 days by MTT assay, IC50 = 0.1 μM.	22480495
HT-29	Cytostatic assay		4 days	Cytostatic activity against human HT-29 cells after 4 days by MTT assay, IC50 = 0.2 μM.	22480495
MCF7	Cytostatic assay		4 days	Cytostatic activity against human MCF7 cells after 4 days by MTT assay, IC50 = 0.4 μM.	22480495
HepG2	Function assay			HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50 = 2.99 μM.	22586124
THP1	Cytotoxicity assay		72 hrs	Cytotoxicity against PMA-stimulated human THP1 cells after 72 hrs by MTT assay, IC50 = 26.9 μM.	22939695
L5178Y	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse L5178Y cells after 24 hrs by MTT assay, IC50 = 0.3 μM.	23199479
L5178Y	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse L5178Y cells after 24 hrs by MTT assay, IC50 = 0.73 μM.	23199479
L5178Y	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse L5178Y cells expressing p-gp after 24 hrs by MTT assay, IC50 = 2.32 μM.	23199479
L5178Y	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse L5178Y cells expressing p-gp after 24 hrs by MTT assay, IC50 = 7.73 μM.	23199479
DA-3	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse DA-3 cells after 24 hrs by XTT assay, IC50 = 1.9 μM.	24900668
SKOV3	Cytotoxicity assay		24 hrs	Cytotoxicity against human SKOV3 cells after 24 hrs by XTT assay, IC50 = 20.6 μM.	24900668
ES2	Cytotoxicity assay		24 hrs	Cytotoxicity against human ES2 cells after 24 hrs by XTT assay, IC50 = 25.5 μM.	24900668
MCF7	Cytotoxicity assay		24 hrs	Cytotoxicity against human MCF7 cells after 24 hrs by XTT assay, IC50 = 33.9 μM.	24900668
MRC5	Antiproliferative assay			Antiproliferative activity against human MRC5 cells by XTT assay, IC50 = 0.078 μM.	25467291
A549	Antiproliferative assay			Antiproliferative activity against human A549 cells by XTT assay, IC50 = 0.08 μM.	25467291
MDA-MB-231	Antiproliferative assay			Antiproliferative activity against human MDA-MB-231 cells by XTT assay, IC50 = 0.091 μM.	25467291
H1299	Antiproliferative assay			Antiproliferative activity against human H1299 cells by XTT assay, IC50 = 0.096 μM.	25467291
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells by XTT assay, IC50 = 0.65 μM.	25467291
HEK293	Cytotoxicity assay		24 hrs	Cytotoxicity against HEK293 cells assessed as cell viability after 24 hrs by Alamar Blue assay, IC50 = 12.55 μM.	26937828
MCF7/ADR	Growth inhibition assay		48 hrs	Growth inhibition of human MCF7/ADR cells after 48 hrs by SRB assay, IC50 = 7.12 μM.	28246041
HCT16	Cytotoxicity assay		72 hrs	Cytotoxicity in human HCT16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay, IC50 = 0.21 μM.	28923382
A549	Cytotoxicity assay		72 hrs	Cytotoxicity in human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay, IC50 = 0.51 μM.	28923382
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay, IC50 = 1.44 μM.	28923382
RD	Cytotoxicity assay		72 hrs	Cytotoxicity in human RD cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay, IC50 = 2.45 μM.	28923382
HEK293	Cytotoxicity assay		72 hrs	Cytotoxicity in human HEK293 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay, IC50 = 11.17 μM.	28923382
CCRF-CEM	Growth inhibition assay			In vitro growth inhibitory activity against CCRF-CEM (human lymphoblastic leukemic) cells, ID50 = 0.04 μM.	6951049
CCRF-CEM	Function assay			Inhibitory activity against CCRF-CEM(human leukemic lymphoblastic) cells in culture, ID50 = 0.04 μM.	7057426
Sf9	Function assay			TP_TRANSPORTER: ATP hydrolysis in membrane vesicle from BCRP-expressing Sf9 cells, Kact = 2.5 μM.	11437380
GLC4/ADR	Function assay			TP_TRANSPORTER: inhibition of DNP-SG uptake in membrane vesicles from GLC4/ADR cells, Ki = 0.95 μM.	9188796
SR3A	Function assay			TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicles from SR3A cells, Ki = 0.07 μM.	9647783
Caco-2	Function assay			TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells, Ki = 2.5 μM.	11405287
MDCK	Function assay			TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells, Ki = 49.4 μM.	12134946
GLC4/ADR	Function assay			TP_TRANSPORTER: efflux in GLC4/ADR cells, Km = 1.4 μM.	7945406
BTI-TN5B1-4	Function assay			TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km = 1.74 μM.	11785684
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, LC50 = 0.35 μM.	19968258
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay, LC50 = 0.86 μM.	19968258
CEM	Cytotoxicity assay		72 hrs	Cytotoxicity against CEM cells after 72 hrs, TCS50 = 0.062 μM.	17608396
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against MCF7 cells after 72 hrs, TCS50 = 0.14 μM.	17608396
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against K562 cells after 72 hrs, TCS50 = 0.23 μM.	17608396
HOS	Cytotoxicity assay		72 hrs	Cytotoxicity against HOS cells after 72 hrs, TCS50 = 0.33 μM.	17608396
G361	Cytotoxicity assay		72 hrs	Cytotoxicity against human G361 cells after 72 hrs, TCS50 = 0.67 μM.	17608396
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against HeLa cells after 72 hrs, TCS50 = 0.67 μM.	17608396
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay, TGI = 0.12 μM.	19968258
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, TGI = 0.17 μM.	19968258
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by sulforhodamine B assay, TGI = 0.33 μM.	19968258
K562	Function assay			Increase in the level of drug uptake in Dox-resistant K562 cells in presence of cyclosporine over its absence	16451059
K562	Function assay			Increase in the level of drug efflux in Dox-resistant K562 cells in presence of cyclosporine over its absence	16451059
KB	Apoptosis assay	1 uM	24 hrs	Induction of apoptotic activity in human KB cells at 1 uM after 24 hrs	18680275
DU145	Function assay	90 nM	72 hrs	Inhibition of topoisomerase 2 in human DU145 cells assessed as stabilization of enzyme-DNA cleavage complex at 90 nM after 72 hrs by immunoblot analysis	22260166
DU145	Function assay	90 nM	30 mins	Inhibition of topoisomerase 2 in human DU145 cells assessed as stabilization of enzyme-DNA cleavage complex at 90 nM after 30 mins by immunoblot analysis	22260166
DU145	Function assay	500 nM	4 hrs	Inhibition of HDAC6-mediated tubulin acetylation in human DU145 cells at 500 nM after 4 hrs by Western blot analysis	22260166
DU145	Function assay	0.1 to 0.5 uM	24 hrs	Inhibition of HDAC in human DU145 cells assessed as histone H3 hyperacetylation at 0.1 to 0.5 uM after 24 hrs by Western blot analysis	22260166
DA-3	Cytotoxicity assay	20 uM	60 mins	Cytotoxicity against mouse DA-3 cells assessed as reduction in cell viability at 20 uM after 60 mins by XTT assay	24900668
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
P388	Antitumor assay	0.25 to 10 mg/kg		Antitumor activity against mouse P388 cells allografted in mouse assessed as tumor growth inhibition at 0.25 to 10 mg/kg	1255661
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Información química, almacenamiento y estabilidad

Peso molecular	563.98	Fórmula	C₂₇H₂₉NO₁₀ . HCl	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	23541-50-6	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Rubidomycin HCl, RP 13057 HCl			Smiles	CC1C(C(CC(O1)OC2CC(CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)C)O)N)O.Cl

Solubilidad

In vitro
Lote:

DMSO : 100 mg/mL (177.31 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 100 mg/mL

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.
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	Saline Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	30.000mg/ml (53.19mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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.

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	DNA synthesis (Cell-free assay) 20 nM(Ki)
In vitro	A concentraciones de fármaco que reflejan la concentración plasmática máxima después de la administración de Daunorubicin, el mecanismo principal probablemente sea a través de la interacción con la topoisomerase II, lo que puede ser un evento desencadenante primario para la detención del crecimiento y/o la muerte celular a través de una vía de señalización que conduce a la apoptosis, al menos en células leucémicas y timocitos. La estructura de quinona permite que la daunorubicina actúe como aceptora de electrones en reacciones mediadas por enzimas oxorreductivas, incluyendo la citocromo P450 reductasa, la NADH deshidrogenasa y la xantina oxidasa. A concentraciones de Daunorubicin que superan aproximadamente 2-4 µM, la toxicidad mediada por radicales libres y la reticulación del ADN pueden hacerse evidentes. La Daunorubicin inhibe las síntesis de ADN y ARN en células HeLa en un rango de concentración de 0,2 a 2 µM. La Daunorubicin inhibe las síntesis de ADN en células tumorales de ascitis de Ehrlich en un rango de concentración de 4 µM. La Daunorubic desencadena la apoptosis a concentraciones de 0,5 y 1 µM en células leucémicas humanas HL-60 o U-937. La Daunorubicin estimula la elevación de ceramida y la apoptosis en células P388 y U937 a través de la síntesis de novo mediante la activación de la enzima ceramida sintasa. La Daunorubicin aumenta de forma dosis-dependiente la exposición a fosfatidilserina y la actividad procoagulante consecuente de las células endoteliales de la vena umbilical humana. La Daunorubicin (0,2 mM) mejora significativamente la liberación de micropartículas endoteliales que son altamente procoagulantes en las células endoteliales de la vena umbilical humana.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/10075079/ [2] https://pubmed.ncbi.nlm.nih.gov/7634330/ [3] https://pubmed.ncbi.nlm.nih.gov/20886178/ [4] https://pubmed.ncbi.nlm.nih.gov/18676016/ [5] https://pubmed.ncbi.nlm.nih.gov/35385754/ [6] https://pubmed.ncbi.nlm.nih.gov/20888384/ [7] https://pubmed.ncbi.nlm.nih.gov/15517865/

Aplicaciones

Métodos	Biomarcadores	PMID
Western blot	p-Chk1 / Chk1 / p-ATR / ATR	26727128
Immunofluorescence	p-Chk1	26727128
Growth inhibition assay	Cell viability	30745844

Información del ensayo clínico

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT04562792	Completed	Relapsed Pediatric ALL\|Relapsed Pediatric AML\|Refractory Acute Myeloid Leukemia\|Refractory Acute Lymphoblastic Leukemia	Children''s Mercy Hospital Kansas City	May 8 2020	Phase 2
NCT03878927	Terminated	Acute Myeloid Leukemia	Weill Medical College of Cornell University\|Jazz Pharmaceuticals\|Pfizer	August 23 2019	Phase 1
NCT03896269	Recruiting	Blasts 10-19 Percent of Bone Marrow Nucleated Cells\|Blasts More Than 5 Percent of Bone Marrow Nucleated Cells\|High Risk Chronic Myelomonocytic Leukemia\|Recurrent Chronic Myelomonocytic Leukemia\|Recurrent High Risk Myelodysplastic Syndrome\|Refractory Chronic Myelomonocytic Leukemia\|Refractory High Risk Myelodysplastic Syndrome	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	May 14 2019	Phase 1

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