Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer)
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。
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包装价格促销价数量
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5mg￥5875.004700.00- +
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10mg￥9087.007270.00- +
- 货号: ajcx13542
- CAS: N/A
- 别名:
- 分子式: C18H18FN5O2S
- 分子量: 387.43
- 纯度: ＞98%
- 溶解度: DMSO : ≥ 113 mg/mL (291.67 mM)
- 储存: 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.
