化合物 T29018
- CAS号:1527513-89-8
- 英文名:(Diphenyl-2-thienylphosphine-κP)[2-(4-methoxyphenyl)ethynyl]gold
- 中文名:化合物 T29018
- CBNumber:CB64902577
- 分子式:C25H21AuOPS
- 分子量:597.44
- MOL File:1527513-89-8.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
化合物 T29018性质、用途与生产工艺
- 生物活性 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。
-
靶点
EC50: 2.8 nM (TrxR)
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体外研究
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
Cell Line: MCF-7 and HT-29 cells Concentration: 0.1, 0.5, 1 μM Incubation Time: 72 hours Result: Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM. Apoptosis Analysis
Cell Line: MCF-7 cells Concentration: 0.8 μM Incubation Time: 4 and 8 hours Result: 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. -
体内研究
TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) effectively 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.
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