For research use only. Not for therapeutic Use.
ASTX-660 (CAT: I022567) is an orally bioavailable non-peptidomimetic antagonist that targets both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular inhibitor of apoptosis protein 1 (cIAP1). It exhibits potential antineoplastic and pro-apoptotic activities. By selectively binding to and inhibiting XIAP and cIAP1, ASTX-660 restores and enhances apoptotic signaling pathways in cancer cells. This leads to the inactivation of the nuclear factor-kappa B (NF-kB)-mediated survival pathway. XIAP and cIAP1 are frequently overexpressed in various cancer types, where they contribute to the suppression of apoptosis and promote cancer cell survival as well as resistance to chemotherapy. ASTX-660 offers a promising approach for targeting XIAP and cIAP1, thereby promoting apoptosis and potentially overcoming chemotherapy resistance in cancer therapy.
| Catalog Number | I022567 |
| CAS Number | 1799328-86-1 |
| Synonyms | ASTX660; ASTX-660; ASTX 660; Tolinapant; Tolinapantum; |
| Molecular Formula | C30H42FN5O3 |
| Purity | 98% |
| Target | IAP; Apoptosis |
| Solubility | Soluble in DMSO, not in water |
| Appearance | Solid powder |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| IUPAC Name | 1-(6-(4-fluorobenzyl)-5-(hydroxymethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-2-((2R,5R)-5-methyl-2-(((R)-3-methylmorpholino)methyl)piperazin-1-yl)ethan-1-one |
| InChI | InChI=1S/C30H42FN5O3/c1-20-14-35(25(13-32-20)15-34-9-10-39-18-21(34)2)16-28(38)36-19-30(3,4)29-27(36)12-23(26(17-37)33-29)11-22-5-7-24(31)8-6-22/h5-8,12,20-21,25,32,37H,9-11,13-19H2,1-4H3/t20-,21-,25-/m1/s1 |
| InChIKey | YCXOHEXZVKOGEV-DNRQZRRGSA-N |
| SMILES | OCC1=NC2=C(N(CC2(C)C)C(CN3[C@@H](CN4[C@H](C)COCC4)CN[C@H](C)C3)=O)C=C1CC5=CC=C(F)C=C5 |
| Reference | 1: Xiao R, An Y, Ye W, Derakhshan A, Cheng H, Yang X, Allen C, Chen Z, Schmitt NC, Van Waes C. Dual Antagonist of cIAP/XIAP ASTX660 Sensitizes HPV- and HPV+ Head and Neck Cancers to TNFα, TRAIL, and Radiation Therapy. Clin Cancer Res. 2019 Nov 1;25(21):6463-6474. doi: 10.1158/1078-0432.CCR-18-3802. Epub 2019 Jul 2. PMID: 31266830; PMCID: PMC6825532. |
