LDC4297

Alias: LDC044297; LCD-044297; LCD 044297; LDC4297; LDC-4297; LDC 4297
Cat No.:V2731 Purity: ≥98%
LDC4297 is a novel and potentCDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13±0.06 nM for CDK7and IC50s between 10 nM and 10,000 nM for all other analyzed CDKs.
LDC4297 Chemical Structure CAS No.: 1453834-21-3
Product category: CDK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
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Other Forms of LDC4297:

  • LDC4297 hydrochloride
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

LDC4297 is a novel and potent CDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13±0.06 nM for CDK7 and IC50s between 10 nM and 10,000 nM for all other analyzed CDKs. Cyclin-dependent protein kinase 7 (CDK7) regulates transcription and the cell cycle, two processes that are linked to viral replication in many different ways. LDC4297's affinity for CDK7 turns out to be incredibly high. LDC4297 inhibits HCMV replication in cultured primary human fibroblasts (HFFs) in a concentration-dependent manner, with an efficient 50% concentration (EC50) of 24.5 ± 1.3 nM. Interestingly, at submicromolar concentrations, CDK7 inhibition by LDC4297 is not linked to general cytotoxicity. In conclusion, the CDK7 inhibitor LDC4297 is a promising candidate for additional research into antiviral drugs, potentially providing fresh choices for an all-encompassing strategy of antiviral treatment.

Biological Activity I Assay Protocols (From Reference)
Targets
CDK7 (IC50 = 0.13 nM); HSV-1 (IC50 = 0.02 μM); HSV-2 (IC50 = 0.27 μM)
ln Vitro

In vitro activity: LDC4297 inhibits CDK7 in vitro in the nano-picomolar range. LDC4297 demonstrates a very high affinity for CDK7. LDC4297 inhibits HCMV replication in cultured primary human fibroblasts (HFFs) in a concentration-dependent manner, with an effective concentration (EC50) of 24.5 ± 1.3 nM. Interestingly, at submicromolar concentrations, LDC4297's inhibition of CDK7 is not linked to any general cytotoxicity. In contrast, LDC4297 causes cytotoxicity in a subset of tumor cell lines, sometimes even at incredibly low nanomolar concentrations. Via a complex mechanism of action that includes interfering with virus-induced Rb phosphorylation, LDC4297 exhibits anti-HCMV activity[1].

ln Vivo
The PK analyses of LDC4297 that have been completed so far show great promise as well. Positive characteristics are revealed after oral administration of a single-dose treatment (100 mg/kg of LDC4297) in CD1 mice, according to an analysis of the PK parameters. LDC4297 plasma levels are present for at least 8 hours and have a bioavailability of 97.7%. The half-life (t1/2z) is found to be 1.6 hours, and the time (Tmax) to a mean peak plasma concentration of 1,297.6 ng/ml is reached 0.5 h after administration[1].
Enzyme Assay
LDC4297 is a newly developed and highly effective inhibitor of CDK7 (Cyclin-dependent protein kinase 7), with an IC50 of 0.13±0.06 nM for CDK7 and IC50s ranging from 10 nM to 10,000 nM for all other CDKs examined. Cyclin-dependent protein kinase 7 (CDK7) regulates transcription and the cell cycle, two processes that are linked to viral replication in many different ways. LDC4297's affinity for CDK7 turns out to be incredibly high. LDC4297 inhibits HCMV replication in cultured primary human fibroblasts (HFFs) in a concentration-dependent manner, with an efficient 50% concentration (EC50) of 24.5 ± 1.3 nM. Interestingly, at submicromolar concentrations, CDK7 inhibition by LDC4297 is not linked to general cytotoxicity. In conclusion, the CDK7 inhibitor LDC4297 is a promising candidate for additional research into antiviral drugs, potentially providing fresh choices for an all-encompassing strategy of antiviral treatment.
Cell Assay
Cultured cells seeded in 24-well plates are used for a trypan blue exclusion assay. The cells are incubated with increasing concentrations of antiviral compounds (ranging from 0.1 to 50 μM) for the indicated durations. After 10 minutes at room temperature and cell staining with 0.1% trypan blue, the percentage of viable cells is calculated by microscopic counting.
Animal Protocol
CD1 mice[1]
100 mg/kg
Oral gavage; 100 mg/kg once
References

[1]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H28N8O
Molecular Weight
432.52
Exact Mass
432.24
Elemental Analysis
C, 63.87; H, 6.53; N, 25.91; O, 3.70
CAS #
1453834-21-3
Appearance
Solid powder
SMILES
CC(C)C1=C2N=C(N=C(N2N=C1)NCC3=CC=CC=C3N4C=CC=N4)OC5CCCNC5
InChi Key
LSGRZENCFIIHNV-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H28N8O/c1-16(2)19-15-27-31-21(19)28-23(32-18-8-5-10-24-14-18)29-22(31)25-13-17-7-3-4-9-20(17)30-12-6-11-26-30/h3-4,6-7,9,11-12,15-16,18,24H,5,8,10,13-14H2,1-2H3,(H,25,28,29)
Chemical Name
2-piperidin-3-yloxy-8-propan-2-yl-N-[(2-pyrazol-1-ylphenyl)methyl]pyrazolo[1,5-a][1,3,5]triazin-4-amine
Synonyms
LDC044297; LCD-044297; LCD 044297; LDC4297; LDC-4297; LDC 4297
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~86 mg/mL (~198.8 mM)
Water: <1 mg/mL
Ethanol: ~86 mg/mL (~198.8 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • LDC4297

    Chemical structure and selectivity profile of LDC4297.



    LDC4297

    Inhibitory effect of LDC4297 on individual stages of viral gene expression.Antimicrob Agents Chemother.2015 Apr;59(4):2062-71.
  • LDC4297

    Inhibitory activity of LDC4297 regarding HCMV replication and cell proliferation.Antimicrob Agents Chemother.2015 Apr;59(4):2062-71.
  • LDC4297

    LDC4297 exerts differential impact on the expression levels of several cellular and viral proteins.



    LDC4297

    In vitro kinase activity of pUL97 is not inhibited by LDC4297.Antimicrob Agents Chemother.2015 Apr;59(4):2062-71.
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