ASTX660 hydrochloride

Modify Date: 2023-01-10 22:27:43

ASTX660 hydrochloride Structure
ASTX660 hydrochloride structure
Common Name ASTX660 hydrochloride
CAS Number 1799328-50-9 Molecular Weight 612.612
Density N/A Boiling Point N/A
Molecular Formula C30H44Cl2FN5O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ASTX660 hydrochloride


ASTX660 hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts. Blood Cancer Phase 2 Clinical

 Names

Name ASTX660 hydrochloride

 ASTX660 hydrochloride Biological Activity

Description ASTX660 hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts. Blood Cancer Phase 2 Clinical
References References 1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017. View Related Products by Target IAP Blood Cancer

 Chemical & Physical Properties

Molecular Formula C30H44Cl2FN5O3
Molecular Weight 612.612