LCL-161
LCL-161 is a second mitochondria-derived activator of caspases (SMAC) mimetic that binds to cIAP1 and cIAP2 (members of the inhibitors of apoptosis family of proteins, often upregulated in many cancers) and initiates their destruction. This compound exhibits anticancer chemotherapeutic activity by inducing apoptosis in in vitro models of lymphoid cancers. LCL-161 also activates human PXR and induces activity of CYP3A4/5.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18937970
| Cas No. |
1005342-46-0 |
|---|---|
| Purity |
≥99%, ≥99%ee, de |
| Formula |
C26H33FN4O3S |
| Formula Wt. |
500.63 |
| IUPAC Name |
(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide |
| Synonym |
LCL161 |
| Solubility |
In DMSO |
| Appearance |
white powder |
Dhuria S, Einolf H, Mangold J, et al. Time-dependent inhibition and induction of human cytochrome P4503A4/5 by an oral IAP antagonist, LCL161, in vitro and in vivo in healthy subjects. J Clin Pharmacol. 2013 Jun;53(6):642-53. PMID: 23585187.
Houghton PJ, Kang MH, Reynolds CP, et al. Initial testing (stage 1) of LCL161, a SMAC mimetic, by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2012 Apr;58(4):636-9. PMID: 21681929.
