1. Cell Cycle/DNA Damage
    Anti-infection
  2. CDK
    HSV
  3. LDC4297

LDC4297 

Cat. No.: HY-12653 Purity: 99.14%
Handling Instructions

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

For research use only. We do not sell to patients.

LDC4297 Chemical Structure

LDC4297 Chemical Structure

CAS No. : 1453834-21-3

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10 mM * 1 mL in DMSO USD 114 In-stock
Estimated Time of Arrival: December 31
2 mg USD 80 In-stock
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5 mg USD 120 In-stock
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10 mg USD 190 In-stock
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25 mg USD 390 In-stock
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50 mg USD 690 In-stock
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100 mg USD 1200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

CDK7

0.13 nM (IC50)

HSV-1

0.02 μM (EC50)

HSV-2

0.27 μM (EC50)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

432.52

Formula

C₂₃H₂₈N₈O

CAS No.

1453834-21-3

SMILES

CC(C)C1=C(N2N=C1)N=C(OC3CNCCC3)N=C2NCC4=CC=CC=C4N5C=CC=N5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (138.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3120 mL 11.5602 mL 23.1203 mL
5 mM 0.4624 mL 2.3120 mL 4.6241 mL
10 mM 0.2312 mL 1.1560 mL 2.3120 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

LDC4297LDC 4297LDC-4297CDKHSVCyclin dependent kinaseHerpes simplex virusInhibitorinhibitorinhibit

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