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ASTX660

Chemical Structure : ASTX660

CAS No.: 1799328-86-1

ASTX660 (Tolinapant, ASTX 660, ASTX-660)

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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 539.696
Formula C30H42FN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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

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