[CAS NO. 2699091-15-9] CDK4/6-IN-14
PRODUCTS SPECIFICATIONS [2699091-15-9]
DESCRIPTION [2699091-15-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 483.97 |
| Molecular Formula | C24H27ClFN7O |
| SMILES | O=C1N(CC)CCC2=C1C=CC(C3=NC(NC4=NC=C(N5CCNCC5)C=C4)=NC=C3F)=C2.Cl |
Summary
IC50 & Target
|
CDK4 10 nM (IC 50 ) |
CDK6 16 nM (IC 50 ) |
CDK1 >10000 nM (IC 50 ) |
CDK2 1045 nM (IC 50 ) |
CDK7 2595 nM (IC 50 ) |
CDK9 2664 nM (IC 50 ) |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. | C max (ng/mL) | AUC 0-∞ (h × ng/mL) | MRT 0-∞ (h) | T max (h) | t 1/2 (h) | F (%) |
| IV | 290.52 | 372.56 | 3.50 | 0.033 | 2.62 | |
| PO | 144.11 | 1612.18 | 9.11 | 6 | 3.59 | 43 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.