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LY2857785

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Chemical Structure| 1619903-54-6 同义名 : -
CAS号 : 1619903-54-6
货号 : A732116
分子式 : C26H36N6O
纯度 : 99%+
分子量 : 448.604
MDL号 : MFCD28167812
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(20.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CDK8

    CDK8, IC50:0.016 μM

  • CDK9

    CDK9, IC50:0.011 μM

  • CDK7

    CDK7, IC50:0.246 μM
描述 LY2857785 exhibits high specificity against a panel of 114 protein kinases, inhibiting only 5 others with an IC50 under 0.1 μM, and a total of 14 kinases below 1 μM. At the cellular level, in U2OS cells, it blocks CTD P-Ser2 and CTD P-Ser5 with IC50s of 0.089 (n=13) and 0.042 (n=1) μM, respectively. Yet, LY2857785 only slightly increases G2-M DNA content from 35% to 55%, with an EC50 of 0.135 μM. The compound demonstrates strong, exposure- and time-dependent inhibition of cell proliferation in MV-4-11, RPMI8226, and L363 cell lines. With 4 to 24 hours of incubation, maximal inhibition occurs at 8 hours, with IC50 values of 0.04, 0.2, and 0.5 μM for MV-4-11, RPMI8226, and L363 cells, respectively. LY2857785 also induces time-dependent apoptosis in cancer cells, reaching peak effectiveness at 8 hours with an IC50 of 0.5 μM in L363 cells[1].
作用机制 LY2857785 is a competitive ATP kinase inhibitor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.15mL

2.23mL

1.11mL

22.29mL

4.46mL

2.23mL
参考文献

[1]Yin T, et al. A novel CDK9 inhibitor shows potent antitumor efficacy in preclinical hematologic tumor models. Mol Cancer Ther. 2014 Jun;13(6):1442-56. Mol Cancer Ther. 2014 Jun;13(6):1442-56.