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Chemical Structure : ASTX660
CAS No.: 1799328-86-1
Catalog No.: PC-63391Not For Human Use, Lab Use Only.
Tolinapant (ASTX660) is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $288 | In stock | |
| 50 mg | $498 | In stock | |
| 100 mg | $798 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Tolinapant (ASTX660) is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
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 cell.
ASTX660 induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent.
ASTX660 inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.
| M.Wt | 539.696 | |
| Formula | C30H42FN5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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 |
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1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017.
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