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LDC4297

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Chemical Structure| 1453834-21-3 同义名 : LDC044297
CAS号 : 1453834-21-3
货号 : A162429
分子式 : C23H28N8O
纯度 : 99%+
分子量 : 432.521
MDL号 : MFCD28411427
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(138.72 mM)，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

  • CDK7

    CDK7, IC50:0.13 nM
描述 Cyclin-dependent protein kinase 7 (CDK7) plays an important role in cellular metabolism and viability. LDC4297 is a selective CDK7 inhibitor with an IC50 value of 0.13±0.06nM. It dose-dependently inhibited the replication of human cytomegalovirus in primary human fibroblasts with an EC50 value of 24.5±1.3nM. LDC4297 at 0.37μM reduced Rb expression in uninfected control cells at 24-h post-treatment. In a selection of human-pathogenic Alpha- and Gammaherpesvirinae, LDC4297 blocked virus replication with EC50 values ranging from 0.02-1.21μM. The half-life of LDC4297 (p.o., a single dose of 100mg/kg) in CD1 mice was 1.6h and the time to a mean peak plasma concentration was 1,297.6ng/mL.[3]
作用机制 LDC4297 is a CDK7 inhibitor with antiviral activity at low concentrations.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL
参考文献

[1]Hutterer C, Eickhoff J, et al. A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations. Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71.

[2]Kelso TW, Baumgart K, et al. Cyclin-dependent kinase 7 controls mRNA synthesis by affecting stability of preinitiation complexes, leading to altered gene expression, cell cycle progression, and survival of tumor cells. Mol Cell Biol. 2014 Oct 1;34(19):3675-88.

[3]Hutterer C, Eickhoff J, Milbradt J, et al. A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations. Antimicrob Agents Chemother. 2015;59(4):2062-2071. doi:10.1128/AAC.04534-14