CDK7-IN-8
CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models.
For research use only. We do not sell to patients.
- CAS No.: 2654003-64-0
- Formula: C25H38N8O3
- Molecular Weight:498.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CDK7 54.29 nM (IC50) |
In Vitro
CDK7-IN-8 (0-100 nM; 72 hours) has inhibitory effect on HCC70, OVCAR-3, HCT116 and HCC1806 cells, with IC50 of 50.85 nM, 45.31 nM, 25.26 nM and 44.47 nM respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HCC70, OVCAR-3, HCT116 and HCC1806 cells[1]
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Concentration:0-100 nM
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Incubation Time:72 hours
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Result:Exhibited inhibitory effect on HCC70, OVCAR-3, HCT116 and HCC1806 cells, with IC50 of 50.85 nM, 45.31 nM, 25.26 nM and 44.47 nM respectively.
In Vivo
CDK7-IN-8 (25 mg/kg; p.o., qd, for 21 days) effectively inhibits tumor proliferation with tumor growth inhibition (TGI) value of 81.9%[1].
Pharmacokinetic Parameters of CDK7-IN-8 in male ICR mice[1].
| IG (20 mg/kg) | IG (40 mg/kg) | |
| T1/2 (h) | 1.48 | 2.99 |
| Tmax (h) | 0.50 | 4.67 |
| Cmax (ng/mL) | 3379.92 | 783.01 |
| AUC0-t (h*ng/mL) | 6258.34 | 7828.87 |
| AUC0-∞ (h*ng/mL) | 6375.00 | 7879.45 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice [1]
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Dosage:20 or 40 mg/kg
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Administration:i.g., single (pharmacokinetic analysis)
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Result:Showed good advantages Pharmacokinetic properties.
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Animal Model:Male BALB/c nude mice (injected with HCT116 tumor cells)[1]
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Dosage:25 mg/kg
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Administration:p.o., qd, for 21 days
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Result:Effectively inhibited tumor proliferation with tumor growth inhibition (TGI) value of 81.9%.
Chemical Information
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CAS No. 2654003-64-0
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Molecular Weight 498.62
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Formula C25H38N8O3
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SMILES
CC(C1=C2N(N=C1)C(NC3CCN(CC3)C(O[C@@H]4CN(CC4)C(/C=C/CN(C)C)=O)=O)=NC(C)=N2)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK7-IN-8 Related Classifications
HY-143586 Related Classifications
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