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LDC4297

CAS No. : 1453834-21-3

MCE 站：LDC4297

产品活性：LDC4297是高效和选择性的CDK7抑制剂，IC₅₀值为0.13 nM。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection

作用靶点：CDK  |  HSV

In Vitro: 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 μM 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 μM, respectively) and intermediate to low efficacy for HSV-2 and EBV (EC₅₀s = 0.27 and 1.21 μM, respectively.

In Vivo: 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%.

相关产品：Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Antiviral Compound Library  |  Anti-Aging Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  2-Deoxy-D-glucose  |  Brefeldin A  |  Cytarabine  |  Ro-3306  |  Imiquimod  |  Ivermectin  |  Seliciclib  |  Flavopiridol  |  Salubrinal  |  Ganciclovir  |  NVP-2  |  SNS-032  |  Surfactin  |  AZD-5438  |  Floxuridine  |  Kenpaullone  |  Acyclovir  |  GSK 3 Inhibitor IX  |  AUZ 454  |  XL413 hydrochloride  |  CGP60474  |  Ginsenoside Rb1  |  Wogonin  |  CVT-313  |  Levamisole hydrochloride  |  NG 52  |  Xanthohumol  |  BMS-265246

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