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LDC-4297 HCl (1453834-21-3(free base))

Catalog No. T4417 CAS T4417

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

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LDC-4297 HCl (1453834-21-3(free base)) Chemical Structure

LDC-4297 HCl (1453834-21-3(free base)), CAS T4417

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 77.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 175.00
25 mg	In stock	$ 357.00
50 mg	In stock	$ 529.00
100 mg	In stock	$ 767.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.81%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
Targets&IC50	CDK7:0.13 nM
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%
Cell Research	A trypan blue exclusion assay is performed with cultured cells seeded in 24-well plates and incubated with increasing concentrations of antiviral compound LDC4297 (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

Molecular Weight	469.02
Formula	C23H29ClN8O
CAS No.	T4417

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (127.93 mM)

References and Literature

1. Hutterer C,etal. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Cell Cycle Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Cancer Compound Library NO PAINS Compound Library Kinase Inhibitor Library Bioactive Compound Library

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Keywords

LDC-4297 HCl (1453834-21-3(free base)) T4417 Cell Cycle/Checkpoint CDK LDC4297 HCl (1453834213(free base)) LDC 4297 HCl (1453834 21 3(free base)) inhibitor inhibit

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