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LDC4297 CDK inhibitor

Cat.No.S7992

LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).
LDC4297 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 432.52

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Quality Control

Batch: S799201 DMSO]86 mg/mL]false]Ethanol]86 mg/mL]false]Water]Insoluble]false Purity: 99.51%
99.51

Chemical Information, Storage & Stability

Molecular Weight 432.52 Formula

C23H28N8O

 Storage (From the date of receipt)
CAS No. 1453834-21-3 Download SDF Storage of Stock Solutions

Synonyms LDC044297 Smiles CC(C)C1=C2N=C(N=C(N2N=C1)NCC3=CC=CC=C3N4C=CC=N4)OC5CCCNC5

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (198.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
CDK7 [1]
(Cell-free assay)
0.13 nM
In vitro
LDC4297 inhibits CDK7 in vitro in the nano-picomolar range. The affinity of this compound for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by this chemical in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 ± 1.3 nM. Notably, CDK7 inhibition by this inhibitor is not associated with general cytotoxicity at submicromolar concentrations. In contrast, it induces cytotoxicity in a set of tumor cell lines, i.e., already at extremely low, nanomolar concentrations in specific cases. Anti-HCMV activity of this compound is exerted through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation[1].
In vivo
The PK analyses of LDC4297 performed thus far have also been highly promising. 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 this compound. 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 this chemical's plasma levels for at least 8 h and a bioavailability of 97.7%[1].
References

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