包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
Canonical SMILES | N=[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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |