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BS-194

Chemical Structure : BS-194

CAS No.: 1092443-55-4

BS-194 (BS 194;BS194)

Catalog No.: PC-61917Not For Human Use, Lab Use Only.

BS-194 (BS194) is a potent, selective, orally bioactive CDK2 inhibitor with IC50 of 2.4 nM, displays 140-fold selectivity over CDK7 (IC50=378 nM).

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Biological Activity

BS-194 (BS194) is a potent, selective, orally bioactive CDK2 inhibitor with IC50 of 2.4 nM, displays 140-fold selectivity over CDK7 (IC50=378 nM).
BS-194 weakly inhibits CDK1, CDK5, CDK7, and CDK9 with IC50 of 30, 30, 250, and 90 nM.
BS-194 shows inhibition of the phosphorylation of CDK substrates, Rb and the RNA polymerase II C-terminal domain, down-regulation of cyclins A, E, and D1, and cell cycle block in the S and G2/M phases.
BS-194 inhibits human tumor xenografts and suppresses CDK substrate phosphorylation.

Physicochemical Properties

M.Wt 385.468
Formula C20H27N5O3
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

(2S,3S)-3-[[7-(benzylamino)-3-propan-2-ylpyrazolo[1,5-a]pyrimidin-5-yl]amino]butane-1,2,4-triol

References

1. Hazel P, et al. ChemMedChem. 2017 Mar 7;12(5):372-380.

2. Tripathi SK, et al. J Mol Recognit. 2012 Oct;25(10):504-12.

3. Heathcote DA, et al. J Med Chem. 2010 Dec 23;53(24):8508-22.

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