ASTX660
ASTX660 is an orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptoticctivities. Upon administration, XIAP/cIAP1 antagonist ASTX660 selectively binds to and inhibits the activity of XIAP and cIAP1. This restores and promotes the induction of apoptotic signaling pathways in cancer cells, and inactivates the nuclear factor-kappa B (NF-kB)-mediated survival pathway. XIAP and cIAP1 are overexpressed by many cancer cell types and suppress apoptosis by inhibiting the activity of certain caspases; they promote both cancer cell survival and chemotherapy resistance.
| Chemical | |
|---|---|
| CAS Num | 1605316-16-2 (2HCl salt) |
| Chemical Formula | C30H43Cl2FN4O2 |
| Molecular Weight | 581.5984 |
| IUPAC Chemical Name | 1-(6-(4-fluorobenzyl)-3,3-dimethylindolin-1-yl)-2-((2R,5R)-5-methyl-2-(((R)-3-methylmorpholino)methyl)piperazin-1-yl)ethan-1-one dihydrochloride |
| Elemental Analysis | C, 61.96; H, 7.45; Cl, 12.19; F, 3.27; N, 9.63; O, 5.50 |
| Synonym | ASTX660; ASTX-660; ASTX 660. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | CC1(C)CN(C(CN2C[C@H](NC[C@@H]2CN3CCOC[C@H]3C)C)=O)C4=C1C=CC(CC5=CC=C(F)C=C5)=C4.[H]Cl.[H]Cl |
| Biological | |
| Targets and Effects | Apoptosis Protein inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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