LCL161

LCL161

产品参数

货号 规格 操作
L127178-50mg 咨询
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服务地域:全国

属性:产地:上海; 品牌:阿拉丁 ;货期:现货

上海阿拉丁生化科技股份有限公司

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产品描述产品描述
  • 分子式 C26H33FN4O3S
  • 分子量500.63

属性

溶解性 25°C: DMSO
存贮条件 储存温度-20°C

描述

产品介绍 LCL161,一个SMAC模拟的,能有效地结合并抑制多元IAPs(i.e. XIAP, c-IAP)。Phase 2。
生化机理

Description:
IC50 Value: N/A
LCL161 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

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)-propanamide
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