Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) 是BAY-1143572的S-对映异构体 ,是一种有效的选择性CDK9抑制剂,抑制CDK9/CycT1,IC50为 16 nM。
产品描述
Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is the (S)-enantiomer of BAY-1143572. Atuveciclib S-Enantiomer is a potent and selective CDK9 inhibitor, which inhibits CDK9 / CycT1 with an IC 50 of 16 nM.
体外活性
Atuveciclib (BAY-1143572) S-Enantiomer reveals very similar in vitro properties compared with Atuveciclib (BAY-1143572), 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 (IC 50 CDK9/CycT1: 16 nM) and antiproliferative activity against HeLa cells (IC 50 : 1100 nM) [1].
体内活性
Atuveciclib (BAY-1143572) S-Enantiomer shows blood/plasma ratios of about 1. Relative to Atuveciclib (BAY-1143572), Atuveciclib (BAY-1143572) S-Enantiomer reveals very similar rat PK properties in vivo (CL b : 1.2 L/kg per hour, V ss : 1.2 L/kg, t 1/2 : 0.6 h, F: 53 %) [1].
Cas No.
250279-81-1
分子式
C18H18FN5O2S
分子量
387.43
别名
BAY-1143572 S-Enantiomer;Atuveciclib S-Enantiomer
储存和溶解度
DMSO:113 mg/mL (291.67 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years