LDC4297 |
| رقم الكتالوجGC19219 |
LDC4297 هو مثبط CDK7 قوي وانتقائي مع IC50 من 0.13 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1453834-21-3
Sample solution is provided at 25 µL, 10mM.
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LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
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 uM 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 uM, respectively) and intermediate to low efficacy for HSV-2 and EBV (EC50s = 0.27 and 1.21 uM, respectively[1].
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].
References:
[1]. Hutterer C, et al. 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.
Cell experiment: | 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]. |
References: [1]. Hutterer C, et al. 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. | |
| Cas No. | 1453834-21-3 | SDF | |
| Canonical SMILES | CC(C)C1=C(N2N=C1)N=C(OC3CNCCC3)N=C2NCC4=CC=CC=C4N5C=CC=N5 | ||
| Formula | C23H28N8O | M.Wt | 432.52 |
| الذوبان | DMSO : ≥ 60 mg/mL (138.72 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.312 mL | 11.5602 mL | 23.1203 mL |
| 5 mM | 0.4624 mL | 2.312 mL | 4.6241 mL |
| 10 mM | 0.2312 mL | 1.156 mL | 2.312 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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