2699091-15-9
2699091-15-9 structure
- Name: CDK4/6-IN-14
- Chemical Name: CDK4/6-IN-14
- CAS Number: 2699091-15-9
- Molecular Formula: C24H27ClFN7O
- Molecular Weight: 483.97
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2023-02-07 11:30:28
- Modify Date: 2023-02-07 11:30:28
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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[1].
| Name | CDK4/6-IN-14 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
CDK4:10 nM (IC50) CDK6:16 nM (IC50) CDK1:>10000 nM (IC50) CDK2:1045 nM (IC50) CDK7:2595 nM (IC50) CDK9:2664 nM (IC50) |
| In Vitro | 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]. Cell Cytotoxicity Assay[1] Cell Line: MCF-7 and T47D cells Concentration: 1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells) Incubation Time: 5 days Result: Significantly inhibited growth and clone formation of MCF-7 and T47D cells. Western Blot Analysis[1] Cell Line: MCF-7 and T47D cells Concentration: 1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells) Incubation Time: 24 hours Result: Significantly inhibited the phosphorylation of RB. |
| In Vivo | CDK4/6-IN-14 (compound 42; 100-150 mg/kg; p.o; once a day; for 23 days) significantly inhibits tumor growth of the MCF-7 xenograft model[1]. 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 43Dose: i.v. at 1 mg/kg; p.o. at 10 mg/kg[1] Animal Model: BALB/c nude mice bearing MCF-7 cells[1] Dosage: 100 mg/kg, 150 mg/kg Administration: Orally administertion; once a day; for 23 days Result: Significantly inhibited tumor growth of the MCF-7 xenograft model. |
| References |
| Molecular Formula | C24H27ClFN7O |
|---|---|
| Molecular Weight | 483.97 |