TL-32711
TL-32711 is a Smac mimetic that is currently in clinical trials as a potential treatment for a variety of cancers. TL-32711 inhibits members of the inhibitor of apoptosis protein (IAP) family proteins, inducing degradation of cIAP1 and cIAP2. TL-32711 exhibits anticancer chemotherapeutic activity, inhibiting NF-κB activation and tumor growth in animal models. In acute myelogenous leukemia (AML) cells, this compound induces caspase 8-mediated apoptosis. This compound also improves the efficacy of co-administered antivirals in models of hepatitis B infection.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18976681
| Cas No. |
1260251-31-7 |
|---|---|
| Purity |
≥98% |
| Formula |
C42H56F2N8O6 |
| Formula Wt. |
806.94 |
| IUPAC Name |
(2S)-N-[(2S)-1-[(2R,4S)-2-[[6-fluoro-2-[6-fluoro-3-[[(2R,4S)-4-hydroxy-1-[(2S)-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidin-2-yl]methyl]-1H-indol-2-yl]-1H-indol-3-yl]methyl]-4-hydroxypyrrolidin-1-yl]-1-oxobutan-2-yl]-2-(methylamino)propanamide |
| Synonym |
Birinapant |
| Appearance |
White Crystal Powder |
Ebert G, Allison C, Preston S, et al. Eliminating hepatitis B by antagonizing cellular inhibitors of apoptosis. Proc Natl Acad Sci U S A. 2015 May 5;112(18):5803-8. PMID: 25902530.
Benetatos CA, Mitsuuchi Y, Burns JM, et al. Birinapant(TL32711), a Bivalent Smac Mimetic, Targets TRAF2-associated cIAPs, Abrogates TNF-induced NF-κB Activation and is Active in Patient-Derived Xenograft Models. Mol Cancer Ther. 2014 Feb 21. [Epub ahead of print]. PMID: 24563541.
Carter BZ, Mak PY, Mak DH, et al. Synergistic Targeting of AML Stem/Progenitor Cells With IAP Antagonist Birinapant and Demethylating Agents. J Natl Cancer Inst. 2014 Feb 1;106(2):djt440. PMID: 24526787.
