FLT3/CDK4-IN-1 是一种有效的、高选择性且具有口服活性的FLT3/CDK4双重抑制剂 (FLT3 与 CDK4 的IC50为 7 和 11 nM)。FLT3/CDK4-IN-1 对某些癌细胞具有抗增殖活性，在体内具有良好的抗肿瘤作用。
| 生物活性 | FLT3/CDK4-IN-1 is a potent, high selective and orally activeFLT3/CDK4dual inhibitor (IC50=11 and 7 nM forFLT3andCDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certaincancercells. FLT3/CDK4-IN-1 has good antitumor effectin vivo[1]. |
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体外研究
(In Vitro) | FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50of 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 IC50of 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. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
