ASTX660 mesylate

Modify Date: 2024-01-11 06:34:07

ASTX660 mesylate Structure
ASTX660 mesylate structure
Common Name ASTX660 mesylate
CAS Number 1799328-90-7 Molecular Weight 635.796
Density N/A Boiling Point N/A
Molecular Formula C31H46FN5O6S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ASTX660 mesylate


ASTX660 mesylate 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 mesylate

 ASTX660 mesylate Biological Activity

Description ASTX660 mesylate 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 C31H46FN5O6S
Molecular Weight 635.796