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ASTX660 is an inhibitor of apoptosis proteins found to target BIR3 domain of cIAP1/2 and XIAP through a TNFalpha dependent mechanism in melanoma, breast cancer, and lymphoma cell studies. In a breast cancer xenograft model ASTX660 inhibited tumor growth while displaying no significant adverse effects. Treatment of squamous cell carcinoma xenograft models with combination of ASTX660 and radiotherapy showed synergistic effect of delayed tumor growth.
| Cas No. | 1799328-86-1 |
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| Purity | ≥98% |
| Formula | C30H42FN5O3 |
| Formula Wt. | 539.70 |
| Chemical Name | Ethanone, 1-(6-((4-fluorophenyl)methyl)-2,3-dihydro-5-(hydroxymethyl)-3,3-dimethyl-1H-pyrrolo(3,2-b)pyridin-1-yl)-2-((2R,5R)-5-methyl-2-(((3R)-3-methyl-4-morpholinyl)methyl)-1-piperazinyl)- |
| 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 |
| Synonym | ASTX660, ASTX-660, ASTX 660 |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Ward G, Lewis E, Ahn J, et al. ASTX660, a novel non-peptidomimetic antagonist of cIAP1/2 and XIAP, potently induces TNFalpha-dependent apoptosis in cancer cell lines and inhibits tumor growth. Mol Caner Ther. 2018 Jul;17(7):1381-1391. PMID: 29695633.
Xiao R, An Y, Ye W, et al. Dual antagonist of cIAP/XIAP ASTX660 sensitizes HPV- and HPV+ head and neck cancers to TNFalpha, TRAIL, and radiation therapy. Clin Cancer Res. 2019 Nov 1;25(21):6463-6474. PMID: 31266830.
Ye W, Gunti S, Allen C, et al. ASTX660, an antagonist of cIAP1/2 and XIAP, increases antigen processing machinery and can enhance radiation-induced immunogenic cell death in preclinical models of head and neck cancer. Oncoimmunology. 2020 Jan 9;9(1):1710398. PMID: 32002309.