溶解性 | 25°C: DMSO |
存贮条件 | 储存温度-20°C |
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/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 |
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 |
LCL161,抑制剂
LCL161 (订货以英文为准)
编号:L127178
CAS号:1005342-46-0
分子式:C26H33FN4O3S
分子量:500.63
产品名称 | LCL161 |
中文名称 | LCL161,抑制剂 |
CAS号 | 1005342-46-0 |
分子式(M.F.) | C26H33FN4O3S |
分子量(M.W.) | 500.63 |
储存条件 | -20°C储存 |
标识符号 | https://www.aladdin-e.com/images/ghs/ghs07.jpg |
信号词 | Warning |
危害声明 | H315-H319-H335 |
警示性声明 | P261-P305 + P351 + P338 |
个人防护设备 | dust mask type N95 (US), Eyeshields, Gloves |
WGK德国 | 3 |
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