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ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP, it potently inhibited the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively. ASTX660 induced degradation of cIAP1, with an EC50 of 0.22 nmol/L after 2 hours of treatment. ASTX660 treatment of WSU-DLCL2 cells leads to significant cIAP1 and cIAP2 degradation after 1 and 4 hours. ASTX660 is orally bioavailable in mice and demonstrates prolonged antagonism of XIAP and cIAP1 in vivo.
| Molecular Weight | 539.68 |
| Formula | C30H42FN5O3 |
| CAS Number | 1799328-86-1 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IAP Products |
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