| 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 |
