FLT3/CDK4-IN-1
Modify Date: 2024-01-20 18:23:37
FLT3/CDK4-IN-1 structure
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Common Name | FLT3/CDK4-IN-1 | ||
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| CAS Number | 2762296-44-4 | Molecular Weight | 478.54 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H28F2N8 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of FLT3/CDK4-IN-1FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo[1]. |
| Name | FLT3/CDK4-IN-1 |
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| Description | FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo[1]. |
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| Related Catalog | |
| Target |
CDK4:7 nM (IC50) |
| In Vitro | FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively[1]. FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner[1]. FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116[1]. FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner[1]. Cell Proliferation Assay Cell Line: MV4-11, HCT-116, MDA-MB-436[1] Concentration: Various concentrations Incubation Time: 72 hours Result: FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively. Cell Cycle Analysis Cell Line: MV4-11, HCT-116[1] Concentration: 12.5, 25, 50, 100 and 200 nM Incubation Time: 24 hours Result: Arrested the cell cycle in G1 phase in a concentration-dependent manner. Apoptosis Analysis Cell Line: MV4-11, HCT-116[1] Concentration: 200, 400, 800, 1600 and 3200 nM Incubation Time: 48 hours Result: Induced apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and was more capable in MV4-11 than HCT-116. Western Blot Analysis Cell Line: MV4-11[1] Concentration: 0, 5, 10, 20, 40, 100 nM Incubation Time: 2 hours Result: Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner. |
| In Vivo | FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg[1]. Animal Model: Female nu/nu mice (MV4-11-injected)[1] Dosage: 100 and 200 mg/kg Administration: p.o.; 14 days, once daily Result: Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg. |
| References |
| Molecular Formula | C25H28F2N8 |
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| Molecular Weight | 478.54 |