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LDC4297
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LDC4297图片
CAS NO:1453834-21-3
规格:98%
分子量:432.52
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
CAS:1453834-21-3
分子式:C23H28N8O
分子量:432.52
纯度:98%
存储:Store at -20°C

Background:

LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.


The affinity of LDC4297 for CDK7 proves to be extremely high. Kinase assays performed for CDK1, CDK2, CDK4, CDK6, CDK7, and CDK9 confirms the selective inhibitory activity of LDC4297 for CDK7 in the nano-picomolar range (IC50, 0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). LDC4297 exerts anticytomegaloviral activity. Human cytomegalovirus (HCMV) replication is inhibited by LDC4297 in a concentration-dependent manner with an EC50 value of 24.5±1.3 nM. Inhibition is statistically significant and morphological signs of cytotoxicity only occurrs at concentrations of 3.3 uM or higher. Anti-HCMV activity of LDC4297 is exerted through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation. Virus replication is broadly blocked by LDC4297, whereby the antiviral efficacies varied between the viruses used, i.e., strong efficacy for HSV-1 and VZV (EC50s = 0.02 and 0.06 uM, respectively) and intermediate to low efficacy for HSV-2 and EBV (EC50s = 0.27 and 1.21 uM, respectively[1].


An analysis of the PK parameters in CD1 mice reveals positive characteristics after oral administration, as demonstrated for a single-dose treatment (100 mg/kg of LDC4297). The half-life (t1/2z) is determined to be 1.6 h, and a time (Tmax) to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration, with a continued presence of LDC4297 plasma levels for at least 8 h and a bioavailability of 97.7%[1].


参考文献:
[1]. Hutterer C, 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.