CDK4/6-IN-14
CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases.
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- CAS No.: 2699091-15-9
- 화학식: C24H27ClFN7O
- 분자량:483.97
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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CDK4 10 nM (IC50) |
CDK6 16 nM (IC50) |
CDK1 >10000 nM (IC50) |
CDK2 1045 nM (IC50) |
CDK7 2595 nM (IC50) |
CDK9 2664 nM (IC50) |
CDK4/6-IN-14 (compound 42; 1-6 μM; 5 days) exhibits potent inhibitory activity against the proliferation of breast cancer MCF-7, T47D, and ZR-75-1 cell lines. CDK4/6-IN-14 significantly inhibits growth and clone formation of MCF-7 and T47D cells[1].
CDK4/6-IN-14 (compound 42; 1-6 μM) arrests the cell cycle at the G1 phase of MCF-7 and T47D cells in the dose-dependent manner[1].
CDK4/6-IN-14 (compound 42; 1-6 μM; 24 hours) significantly inhibits the phosphorylation of retinoblastoma (RB), while the expression of RB protein was almost unchanged. In addition, CDK4/6-IN-14 exhibits a concentration-dependent effect to decrease the level of c-MYC and cyclin D1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 and T47D cells
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Concentration:1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells)
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Incubation Time:5 days
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Result:Significantly inhibited growth and clone formation of MCF-7 and T47D cells.
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Cell Line:MCF-7 and T47D cells
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Concentration:1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells)
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Incubation Time:24 hours
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Result:Significantly inhibited the phosphorylation of RB.
CDK4/6-IN-14 (compound 42) exhibits a suitable t1/2 of intravenous and oral administration (2.62 and 3.59 h, respectively). Moreover, the oral bioavailability of CDK4/6-IN-14 is 43%[1].
Pharmacokinetic Parameters of CDK4/6-IN-14 (Compound 42) in Sprague–Dawley Rats[1].
| admin. | Cmax (ng/mL) | AUC0-∞ (h × ng/mL) | MRT0-∞ (h) | Tmax (h) | t1/2 (h) | F (%) |
| IV | 290.52 | 372.56 | 3.50 | 0.033 | 2.62 | |
| PO | 144.11 | 1612.18 | 9.11 | 6 | 3.59 | 43 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice bearing MCF-7 cells[1]
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Dosage:100 mg/kg, 150 mg/kg
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Administration:Orally administertion; once a day; for 23 days
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Result:Significantly inhibited tumor growth of the MCF-7 xenograft model.
Chemical Information
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CAS No. 2699091-15-9
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분자량 483.97
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화학식 C24H27ClFN7O
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SMILES
O=C1N(CC)CCC2=C1C=CC(C3=NC(NC4=NC=C(N5CCNCC5)C=C4)=NC=C3F)=C2.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK4/6-IN-14 Related Classifications
HY-151898 Related Classifications
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