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Atuveciclib S-Enantiomer(BAY-1143572 S-Enantiomer)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Atuveciclib S-Enantiomer(BAY-1143572 S-Enantiomer)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
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。
Canonical SMILESN=[S@@](CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O
分子式C18H18FN5O2S
分子量387.43
溶解度DMSO : ≥ 113 mg/mL (291.67 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.