Information Tolinapant (ASTX660) is a potent, non-peptidomimetic antagonist ofcIAP1/2andXIAPthat inhibits 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. Targets cIAP2 ; cIAP1 (Cell-free assay); XIAP (Cell-free assay) ; 12 nM; 40 nM In vitro ASTX660 induces proteasomal degradation of cIAP1 and 2, resulting in downstream effects of NIK stabilization and activation of noncanonical NF-kB signaling, demonstrating cIAP1/2 antagonism. Because of their roles in the evasion of apoptosis, inhibitor of apoptosis proteins (IAP) are considered attractive targets for anticancer therapy. Treatment with ASTX660 leads to TNFa-dependent induction of apoptosis in various cancer cell lines in vitro. In vivo ASTX660 is orally bioavailable in mice and demonstrates prolonged antagonism of XIAP and cIAP1 in vivo. ASTX660 dosing in mice bearing breast and melanoma tumor xenografts causes growth inhibition of MDA-MB-231 and A375 xenograft tumors in vivo. Cell Research(from reference) Cell lines：MDA-MB-231, HEK293, A375, SK-MEL-28, WSU-DLCL2 Concentrations：1 nM - 10 μM Incubation Time：5 min - 4 h
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Tolinapant (ASTX660)
CAS number：1799328-86-1 molecular formula：C3OH42FN5O3
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| Chinese alias | 托利那平 (ASTX660) | ||
| English alias | ASTX 660 | EN300-66089 | 1799328-86-1 | 1-[6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methylmorpholin-4-yl]methyl]piperazin-1-yl]ethanone | ASTX660 | ASTX-660 | MS-29955 | 1-(6-( | ||
| CAS number | 1799328-86-1 | molecular formula | C3OH42FN5O3 |
| molecular weight | 539.68 g/mol | Exact mass | ≥98% |
| PSA | 81.200 Ų | logp | 2.300 |
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