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A-1592668

Chemical Structure : A-1592668

CAS No.: 1628314-13-5

A-1592668 (A 1592668)

Catalog No.: PC-38149Not For Human Use, Lab Use Only.

A-1592668 (A 1592668) is a novel potent, CDK9-selective inhibitor with IC50 of 1.2 nM, >1000 fold selectivity over CDK1/2/7/8.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A-1592668 (A 1592668) is a novel potent, CDK9-selective inhibitor with IC50 of 1.2 nM, >1000 fold selectivity over CDK1/2/7/8.
A-1592668 also displays selectivity of ~12- and 240-fold over CDK4 and CDK6 respectively.
A-1467729 inhibited phosphorylation of RNA pol-II (p-RNA pol-II; Ser2) with a potency of 26.7 nM at the cellular level, inhibited MCL-1 dependent hematologic tumor cell lines H929 (IC50=39 nM) and MV4-11 (IC50=42.4 nM) following 24 h of incubation.

Physicochemical Properties

M.Wt 467.517
Formula C26H27F2N3O3
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

(1r,4r)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-3,6-dihydropyridin-1(2H)-yl)cyclohexane-1-carboxylic acid

References

1. Darren C Phillips, et al. Leukemia. 2020 Jun;34(6):1646-1657.

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