AtuveciclibS-Enantiomer(BAY-1143572S-Enantiomer)是一种有效的选择性CDK9抑制剂，抑制CDK9/CycT1，IC50为16nM。
货号:ajcx30204
CAS:250279-81-1
分子式:C18H18FN5O2S
分子量：387.43
溶解度:DMSO: ≥ 113 mg/mL (291.67 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, which inhibits CDK9/CycT1 with an IC50 of 16 nM.

In comparison with Atuveciclib (BAY-1143572), Atuveciclib (BAY-1143572) S-Enantiomer reveals very similar in vitro properties, well within the limits of measurement accuracy; however, with multiple batches of Atuveciclib (BAY-1143572) S-Enantiomer there is a trend toward a slightly lower activity against CDK9 in the biochemical assay (IC50 CDK9/CycT1: 16 nM) and antiproliferative activity against HeLa cells (IC50: 1100 nM) [1].

Atuveciclib (BAY-1143572) S-Enantiomer exhibits blood/plasma ratios of about 1. Relative to Atuveciclib (BAY-1143572), Atuveciclib (BAY-1143572) S-Enantiomer reveals very similar rat PK properties in vivo (CLb: 1.2 L/kg per hour, Vss: 1.2 L/kg, t1/2: 0.6 h, F: 53 %)[1].

[1]. LÜcking U, et al. Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer. ChemMedChem. 2017 Nov 8;12(21):1776-1793.