Tolinapant (ASTX660) | IAP inhibitor | Probechem Biochemicals

Chemical Structure : ASTX660

CAS No.: 1799328-86-1

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ASTX660 (Tolinapant, ASTX 660, ASTX-660)

货号: 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.

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5 mg	￥1380	In stock
10 mg	￥2180	In stock
25 mg	￥3680	In stock
50 mg	￥5780	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	539.696
分子式	C30H42FN5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017.

ASTX660 (Tolinapant, ASTX 660, ASTX-660)

生物&药学活性

物理化学性质&存储条件

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ASTX660 (Tolinapant, ASTX 660, ASTX-660)

生物&药学活性

物理化学性质&存储条件

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