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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related IAP Products |
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| Sanggenon G
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). |
| TD-1092
TD-1092 is a pan-inhibitor of apoptosis (IAP) degrader with two different types of E3 ligase conjugates, IAP and CRBN, that induces proteasomal degradation of cIAP2 and XIAP in a CRBN-dependent manner. TD1092 also activates apoptotic proteases (apoptosis 3/7) and leads to apoptosis by promoting IAP degradation. In addition, TD1092 also blocks the TNFα-mediated NF-κB signaling pathway and inhibits the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can be used as a PROTAC for cancer research. |
| LBW242
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| UC-112
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| SBP-0636457
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