Pyrrolo[2,1-b][1,3]oxazepine-7-carboxamide, octahydro-8,8-dimethyl-4-[[(2S)-2-(methylamino)-1-oxopropyl]amino]-5-oxo-N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-, (4S,7S,9aS)-

Biological Activity

SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers[1][2]. SBP-0636457 (1-20 μM) demonstrates no cytotoxicity in BT474, BT549, MCF7, and MDA-MB-231 breast cancer cell lines up to a concentration of 20μM[1].SBP-0636457 (10-1000 nM; 20 h) is ef?cacious as TRAIL-sensitizing agents in MDA-MB-231 cells, with an EC50 of 9 nM[1].

References

[1]. Finlay D, et, al. Small-molecule IAP antagonists sensitize cancer cells to TRAIL-induced apoptosis: roles of XIAP and cIAPs. Mol Cancer Ther. 2014 Jan; 13(1): 5-15. [2]. Finlay D, et, al. Inducing death in tumor cells: roles of the inhibitor of apoptosis proteins. F1000Res. 2017 Apr 27; 6:587.