Atuveciclib S-Enantiomer(Synonyms: BAY-1143572 S-Enantiomer)

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Atuveciclib S-Enantiomer (Synonyms: BAY-1143572 S-Enantiomer) 纯度: 99.38%

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) 是一种有效的选择性 CDK9 抑制剂,抑制 CDK9/CycT1IC50 为 16 nM。

Atuveciclib S-Enantiomer(Synonyms: BAY-1143572 S-Enantiomer)

Atuveciclib S-Enantiomer Chemical Structure

CAS No. : 250279-81-1

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10 mg ¥8500 In-stock
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Atuveciclib S-Enantiomer 相关产品

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生物活性

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

IC50 & Target

IC50: 16 nM (CDK9/CycT1)[1]

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

387.43

Formula

C18H18FN5O2S

CAS 号

250279-81-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 113 mg/mL (291.67 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5811 mL 12.9056 mL 25.8111 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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.

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