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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
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.
Targets |
CDK7 (IC50 = 0.13 nM); HSV-1 (IC50 = 0.02 μM); HSV-2 (IC50 = 0.27 μM)
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ln Vitro |
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ln Vivo |
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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.
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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.
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Animal Protocol |
CD1 mice[1]
100 mg/kg Oral gavage; 100 mg/kg once |
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References |
Molecular Formula |
C23H28N8O
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Molecular Weight |
432.52
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Exact Mass |
432.24
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Elemental Analysis |
C, 63.87; H, 6.53; N, 25.91; O, 3.70
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CAS # |
1453834-21-3
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Appearance |
Solid powder
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SMILES |
CC(C)C1=C2N=C(N=C(N2N=C1)NCC3=CC=CC=C3N4C=CC=N4)OC5CCCNC5
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InChi Key |
LSGRZENCFIIHNV-UHFFFAOYSA-N
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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)
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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
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
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.