化合物 T29018
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- CAS号:
- 1527513-89-8
- 英文名:
- (Diphenyl-2-thienylphosphine-κP)[2-(4-methoxyphenyl)ethynyl]gold
- 英文别名:
- TrxR-IN-D9;TrxR inhibitor D9;TrxR inhibitor D-9,TrxR inhibitor D9;(Diphenyl-2-thienylphosphine-κP)[2-(4-methoxyphenyl)ethynyl]gold;(Diphenyl-2-thienylphosphine-κP)[2-(4-methoxyphenyl)ethynyl]gold, ≥98% (HPLC)
- 中文名:
- 化合物 T29018
- 中文别名:
- 化合物 T29018
- CBNumber:
- CB64902577
- 分子式:
- C25H21AuOPS
- 分子量:
- 597.44
- MOL File:
- 1527513-89-8.mol
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化合物 T29018化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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化合物 T29018性质、用途与生产工艺
TrxR inhibitor D9 是一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂，EC50 值为 2.8 nM。TrxR inhibitor D9 具有在体外和体内抑制肿瘤增殖的能力。
TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC
50
s 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 IC
50
s of all cancer cells could be as low as 0.55 μM, and dose not significantly affects 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 significantly 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.
Cell Proliferation Assay
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Cell Line:
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MCF-7 and HT-29 cells
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Concentration:
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0.1, 0.5, 1 μM
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Incubation Time:
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72 hours
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Result:
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Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM.
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Apoptosis Analysis
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Cell Line:
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MCF-7 cells
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Concentration:
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0.8 μM
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Incubation Time:
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4 and 8 hours
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Result:
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Led to more than 50% necrosis/apoptosis of cells compared to control after 4 h of treatment.
Induced all cells necrosis/apoptosis after 8 h of incubation.
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TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice.
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Animal Model:
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BALB/c nude mice (17-18 g) bearing a MCF-7 tumor
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Dosage:
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5 mg/kg
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Administration:
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I.v. once every 2 days for 15 days
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Result:
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Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.
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化合物 T29018
上下游产品信息
上游原料
下游产品
1527513-89-8, 化合物 T29018 相关搜索:
- 抑制剂
- 化合物 T29018
- 1527513-89-8
- TrxR inhibitor D-9,TrxR inhibitor D9
- TrxR-IN-D9
- (Diphenyl-2-thienylphosphine-κP)[2-(4-methoxyphenyl)ethynyl]gold, ≥98% (HPLC)
- TrxR inhibitor D9
- (Diphenyl-2-thienylphosphine-κP)[2-(4-methoxyphenyl)ethynyl]gold