LCL-161
Axon 3902
CAS:
1005342-46-0
- Optical Purity: 100% e.e.
- Soluble in DMSO
- MF: C26H33FN4O3S
- MW: 500.63
Description
LCL-161 is an orally bioavailable and cell permeable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins.
More Information
| Parent CAS No. | 1005342-46-0 |
|---|---|
| Chemical Name | (S)-N-((S)-1-cyclohexyl-2-((S)-2-(4-(4-fluorobenzoyl)thiazol-2-yl)pyrrolidin-1-yl)-2-oxoethyl)-2-(methylamino)propanamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C([C@@H](C(=O)N2[C@H](C3SC=C(C(=O)C4C=CC(F)=CC=4)N=3)CCC2)NC(=O)[C@H](C)NC)CCCC1 |&1:2,6,27,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C26H33FN4O3S/c1-16(28-2)24(33)30-22(17-7-4-3-5-8-17)26(34)31-14-6-9-21(31)25-29-20(15-35-25)23(32)18-10-12-19(27)13-11-18/h10-13,15-17,21-22,28H,3-9,14H2,1-2H3,(H,30,33)/t16-,21-,22-/m0/s1 |
| InChiKey | UFPFGVNKHCLJJO-SSKFGXFMSA-N |
| CID | 24737642 |
| Short Description | IAP inhibitor |
References
- KF Chen et al. Inhibition of Bcl-2 improves effect of LCL161, a SMAC mimetic, in hepatocellular carcinoma cells. Biochem Pharmacol. 2012 Aug 1;84(3):268-77.
- S Dhuria 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.
- Infante JR, Dees EC, Olszanski AJ, Dhuria SV, Sen S, Cameron S, Cohen RB. Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2014 Oct 1;32(28):3103-10.
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