LDC4297

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 2mg
ArtNr HY-12653-2mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Description
LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM. IC50 & Target: IC50: 0.13 nM (CDK7)[1] 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 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]. 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%[1].
CAS No.
1453834-21-3
Purity
>98%
MW
432, 5214
Formula
C23H28N8O
Solubility
DMSO: >=60 mg/mL
Clinical Phase
No Development Reported
Signalling Pathway
Cell Cycle/DNA Damage
Target
CDK
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 2mg
Lieferbar: In stock
Listenpreis: 155,00 €
Preis: 155,00 €
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