1619903-54-6|LY2857785|CsnPharm

CAS No.: 1619903-54-6

LY2857785 Catalog No. CSN17957

Synonyms: LY2857785

LY2857785 is a potent and selective CDK9 inhibitor and significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述LY2857785 is a potent CDK9 inhibitor with IC50 value of 11nM, as well as exhibits CDK8 and CDK7 inhibition with IC50 value of 16nM and 246nM in a SAR study, respectively. LY2857785 inhibited cellular CTDP-Ser2 and CTD P-Ser5, the substrates of CDK9, in U2OS cells at IC50 values of 89nM and 42nM, respectively. Treatment with LY2857785 at concentrations of 0.32, 0.8, 2 and 5μM for 4h led decreased RNAP II CTD phosphorylation in a dose-dependent manner and induced apoptosis measured by PARP cleavage, as well as the antiapoptosis MCL1 and XIAP proteins expression inhibition, in AML patient PBMC cells. Also, LY2857785 led potent in vivo RNAP II CTD P-Ser2 inhibition with TED50 (Threshold Effective Dose) of 4.4mg/kg and TEC50 (Threshold Effective Concentration) of 0.36μM in HCT116 xenograft tumor-bearing mice. LY2857785 demonstrated significant antitumor growth efficacy in AML MV-4-11 xenograft tumor mice model at dose of 18mg/kg (i.v., Q5D×5) in U87MG glioblastoma xenograft tumor model (20 mg/kg, i.v. bolus, Q3D), melanoma A375 xenograft model (20 mg/kg, i.v. bolus, Q3D).
作用机制LY2857785 is a competitive ATP kinase inhibitor.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2291 mL
- 11.1457 mL
- 22.2914 mL
- 5 mM
- 0.4458 mL
- 2.2291 mL
- 4.4583 mL
- 10 mM
- 0.2229 mL
- 1.1146 mL
- 2.2291 mL

技术信息

CAS号

1619903-54-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H36N6O

运输

蓝冰

分子量

448.60

别名

LY2857785

溶解度

DMSO	23.0 mg/mL (51.3 mM)
Water	Insoluble
Ethanol	42.0 mg/mL (93.6 mM)

动物实验配方

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