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LDC4297 CDK inhibitor

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

Purity & Quality Control

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

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Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Mechanism of Action

Targets
CDK7 [1]
(Cell-free assay)
0.13 nM

In vitro
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].
Cell Research Cell lines human fibroblasts
Concentrations 0.1 to 50 μM
Incubation Time 3 days
Method A trypan blue exclusion assay is performed with cultured cells seeded in 24-well plates and incubated with increasing concentrations of antiviral compounds (range, 0.1 to 50 μM) for the durations indicated. Cell staining is achieved with 0.1% trypan blue for 10 min at room temperature before the percentage of viable cells is determined by microscopic counting.

In Vivo
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].
Animal Research Animal Models CD-1 mice
Dosages 100 mg/kg
Administration oral administration

References
  • https://pubmed.ncbi.nlm.nih.gov/25624324/

Chemical Information

Molecular Weight 432.52 Formula

C23H28N8O
CAS No. 1453834-21-3 SDF Download SDF
Synonyms LDC044297
Smiles CC(C)C1=C2N=C(N=C(N2N=C1)NCC3=CC=CC=C3N4C=CC=N4)OC5CCCNC5

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (198.83 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble


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In vivo
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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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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