ASTX660 mesylate( ASTX 660 | ASTX-660 )

Catalog No. M12720 CAS No. 1799328-90-7

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Product Name

ASTX660 mesylate
Note

Research use only, not for human use.
Brief Description

ASTX660 mesylate is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
Description

ASTX660 mesylate is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; 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; 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.Blood Cancer Phase 2 Clinical.
In Vitro

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In Vivo

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Synonyms

ASTX 660 | ASTX-660
Pathway

Apoptosis
Target

IAP
Recptor

IAP
Research Area

Cancer
Indication

Blood cancer

CAS Number

1799328-90-7
Formula Weight

635.796
Molecular Formula

C31H46FN5O6S
Purity

>98% (HPLC)
Solubility

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SMILES

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Chemical 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 methanesulfonate

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

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