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.
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- CAS No.: 2654003-64-0
- Formule: C25H38N8O3
- Masse moléculaire:498.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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.
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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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Masse moléculaire 498.62
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK7-IN-8 Related Classifications
HY-143586 Related Classifications
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