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Chemical Structure : ASTX660 hydrochloride
Catalog No.: PC-63392Not For Human Use, Lab Use Only.
Tolinapant (ASTX660) hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
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Tolinapant (ASTX660) hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
Tolinapant (ASTX660) potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cells.
Tolinapant (ASTX660) induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.
| M.Wt | 612.612 | |
| Formula | C30H44Cl2FN5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017.
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