产品
编 号：F180590
分子式：C25H20AuOPS
分子量：596.43
分子式：C25H20AuOPS
分子量：596.43
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CAS No: 1527513-89-8
产品详情
生物活性：
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
体内研究：
TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) e?ectively inhibits the growth of tumors in mice.Animal Model:BALB/c nude mice (17-18 g) bearing a MCF-7 tumor
Dosage:5 mg/kg
Administration:I.v. once every 2 days for 15 days
Result:Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.
体外研究：
TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC50s of 0.03 and 0.1 μM for MCF-7 and HT-29 cells, respectively.TrxR inhibitor D9 (72 h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60 μM, and the IC50s of all cancer cells could be as low as 0.55 μM, and dose not signi?cantly a?ects normal cells viability.TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis.TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner.TrxR inhibitor D9 (1-1000 nM) does not signi?cantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM.TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin.
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
体内研究：
TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) e?ectively inhibits the growth of tumors in mice.Animal Model:BALB/c nude mice (17-18 g) bearing a MCF-7 tumor
Dosage:5 mg/kg
Administration:I.v. once every 2 days for 15 days
Result:Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.
体外研究：
TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC50s of 0.03 and 0.1 μM for MCF-7 and HT-29 cells, respectively.TrxR inhibitor D9 (72 h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60 μM, and the IC50s of all cancer cells could be as low as 0.55 μM, and dose not signi?cantly a?ects normal cells viability.TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis.TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner.TrxR inhibitor D9 (1-1000 nM) does not signi?cantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM.TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin.
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