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CAS:1005342-46-0|LCL161

发布时间:2022-03-14     作者:德尔塔   分享到:

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产品名称 LCL161 英文名称 LCL161 规格或纯度 ≥99% 别名 LCL-161;LCL 161;(2S)-N-[(1S)-1-Cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2-(methylamino)-propanamide;N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2-(methylamino)-(2S) 英文别名 LCL-161;LCL 161;(2S)-N-[(1S)-1-Cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2-(methylamino)-propanamide;N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2-(methylamino)-(2S) 运输条件 超低温冰袋运输 生化机理 Description:IC50 Value: N/ALCL161 is an oral small molecule antagonist of Inhibitor of Apoptosis Proteins (IAPs) that sensitizes a subset of tumors from diverse lineages to treatment with cytotoxic therapies.in vitro: Huh-7 cells co-treated with LCL161 and SC-2001 showed a significant dose-dependent apoptotic effect demonstrated by sub-G1 assay and cleavage of PARP. Furthermore, the combination index (CI) ofLCL161 and SC-2001 showed a convincing synergism in resistant Huh-7 [1]. Results in human liver microsomes indicated LCL161 inhibited CYP3A in a concentration- and time-dependent manner (KI of 0.797??M and kinact of 0.0803?min(-1) ). LCL161 activated human PXR in a reporter gene assay and induced CYP3A4 mRNA up to ?5-fold in human hepatocytes [2]. LCL161 caused rapid degradation of cIAP1 leading to TNFα secretion, LCL161 did not promote apoptosis significantly. However, LCL161 induced expression of MICA and MICB, ligands for the activating im.Small molecule SMAC mimetic inhibitor of multiple IAP (Inhibitor of apoptosis) family proteins.\xa0 (IC 50 = 10.23 μM). Inhibits cell proliferation and viability in two human hepatocellular carcinoma cells (Hep3B, \xa0IC 50 =\xa010, and PLC5, IC 50 = 19).CAS编号 1005342-46-0 溶解性 25°C: DMSO 储存温度 -20°C储存 分子量 500.63 分子式 C26H33FN4O3S