LDC4297
Based on 11 publication(s) in Google Scholar
LDC4297 is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 value of 0.02-1.21 μM. LDC4297 can be used for the research of infection.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.74%
- No. CAS: 1453834-21-3
- Fòrmula: C23H28N8O
- Peso molecular:432.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Anti-Infection Compound Library
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Publications Citing Use of MedChemExpress (MCE) LDC4297
More- Nat Commun. 2024 Mar 13;15(1):2265. [Abstract]
- J Clin Invest. 2025 Aug 12:e188839. [Abstract]
- Int J Biol Macromol. 2025 Mar:294:139117. [Abstract]
- Front Mol Biosci. 2021 Aug 19;8:697457. [Abstract]
- ChemMedChem. 2025 Aug 25:e202500448. [Abstract]
- Front Oncol. 2021 May 24;11:664848. [Abstract]
- SSRN. 2026 Jun 21.
- bioRxiv. 2025 Oct 11.
- SSRN. 2025 Apr 7.
- Freie Universität Berlin. 2023 Nov 29.
- bioRxiv. 2023 Apr 7.
Actividad biológica
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CDK7 0.13 nM (IC50) |
HSV-1 0.02 μM (EC50) |
HSV-2 0.27 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HFF | CC50 |
6.2 μM
Compound: 78; LDC4297
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Cytotoxicity against HFF cells
Cytotoxicity against HFF cells
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[PMID: 33539089] |
LDC4297 (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50 value of 24.5 nM[1]. LDC4297 (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50 value of 4.5 μM[1]. LDC4297 (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation[1]. LDC4297 (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary cultures of fibroblasts derived from human (HFF) with virus infection
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Concentration:20 μM
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Incubation Time:12, 24, 48 and 96 hours
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Result:Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; 100 mg/kg once
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Result:Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.
Chemical Information
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No. CAS 1453834-21-3
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Appearance Solid
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Peso molecular 432.52
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Fòrmula C23H28N8O
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Color White to off-white
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SMILES
CC(C)C1=C(N2N=C1)N=C(OC3CNCCC3)N=C2NCC4=CC=CC=C4N5C=CC=N5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Commun
High-resolution cryo-EM of the human CDK-activating kinase for structure-based drug design. [Abstract]2024 Mar 13;15(1):2265. PMID: 38480681 -
J Clin Invest
Dual targeting CDK4/6 and CDK7 augments tumor response and anti-tumor immunity in breast cancer models. [Abstract]2025 Aug 12:e188839. PMID: 40794455 -
Int J Biol Macromol
CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609. [Abstract]2025 Mar:294:139117. PMID: 39733900 -
Front Mol Biosci
2021 Aug 19;8:697457. PMID: 34490348 -
ChemMedChem
Novel Pyrazolo [1,5-a]-1,3,5-Triazine Derivatives as CDK7 Inhibitors: Synthesis and Biological Insights in Pancreatic Ductal Adenocarcinoma Models. [Abstract]2025 Aug 25:e202500448. PMID: 40853714 -
Front Oncol
Targeting Mutated p53 Dependency in Triple-Negative Breast Cancer Cells Through CDK7 Inhibition. [Abstract]2021 May 24;11:664848. PMID: 34109118 -
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Solvente y solubilidad
DMSO : ≥ 60 mg/mL (138.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3120 mL | 11.5602 mL | 23.1203 mL | 57.8008 mL |
| 5 mM | 0.4624 mL | 2.3120 mL | 4.6241 mL | 11.5602 mL | |
| 10 mM | 0.2312 mL | 1.1560 mL | 2.3120 mL | 5.7801 mL | |
| 15 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8534 mL | |
| 20 mM | 0.1156 mL | 0.5780 mL | 1.1560 mL | 2.8900 mL | |
| 25 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3120 mL | |
| 30 mM | 0.0771 mL | 0.3853 mL | 0.7707 mL | 1.9267 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4450 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9633 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7225 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL |
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