Home DNA Damage/DNA Repair Antineoplastic and Immunosuppressive Antibiotics inhibitor Daunorubicin HCl

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Daunorubicin HCl Antineoplastic and Immunosuppressive Antibiotics inhibitor

Cat.No.S3035

Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.Daunorubicin (RP 13057) HCl can be used to induce animal models of Kidney Disease.
Daunorubicin HCl Antineoplastic and Immunosuppressive Antibiotics inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 563.98

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Quality Control

Batch: Purity: 99.98%
99.98

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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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Solubility

In vitro
Batch:

DMSO : 100 mg/mL (177.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 563.98 Formula

C27H29NO10 . HCl

 Storage (From the date of receipt)
CAS No. 23541-50-6 Download SDF Storage of Stock Solutions

Synonyms 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

Mechanism of Action

Targets/IC50/Ki
DNA synthesis
(Cell-free assay)
20 nM(Ki)
In vitro

At drug concentrations that reflect the peak plasma concentration after Daunorubicin administration, the primary mechanism is likely to be through interaction with topoisomerase II, which may be a primary triggering event for growth arrest and/or cell killing through a signalling pathway leading to apoptosis, at least in leukemic cells and thymocytes. The quinone structure permits daunorubicin to act as electron acceptors in reactions mediated by oxoreductive enzymes including cytochrome P450 reductase, NADH dehydrogenase, and xanthine oxidase. At Daunorubicin concentrations exceeding approximately 2–4 μM, free radical mediated toxicity and DNA cross-linking may become evident. Daunorubicin inhibits both DNA and RNA syntheses in HeLa cells over a concentration range of 0.2 through 2 μM. Daunorubicin inhibits both DNA syntheses in Ehrlich ascites tumor cells over a concentration range of 4 μM. Daunorubic triggers apoptosis at concentrations of 0.5 and 1 μM in either HL-60 or U-937 human leukemic cells.

Daunorubicin stimulates ceramide elevation and apoptosis in P388 and U937 cells through de novo synthesis via activation of the enzyme ceramide synthase.

Daunorubicin dose-dependently increases the phosphatidylserine exposure and consequent procoagulant activity of human umbilical vein endothelial cells. Daunorubicin (0.2 mM) significantly enhances the release of endothelial microparticles which are highly procoagulant in human umbilical vein endothelial cells.

References
  • [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/

Applications

Methods Biomarkers Images PMID
Western blot p-Chk1 / Chk1 / p-ATR / ATR
S3035-WB1
26727128
Immunofluorescence p-Chk1
S3035-IF1
26727128
Growth inhibition assay Cell viability
S3035-viability1
30745844

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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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