| Identification | Back Directory | [Name]
2-Pyrimidinamine, N-[4-(4-ethyl-1-piperazinyl)-3-fluorophenyl]-5-fluoro-4-[1-(1-methylethyl)-1H-pyrazolo[4,3-b]pyridin-6-yl]- | [CAS]
2762296-44-4 | [Synonyms]
FLT3/CDK4-IN-1
2-Pyrimidinamine, N-[4-(4-ethyl-1-piperazinyl)-3-fluorophenyl]-5-fluoro-4-[1-(1-methylethyl)-1H-pyrazolo[4,3-b]pyridin-6-yl]- | [Molecular Formula]
C25H28F2N8 | [MOL File]
2762296-44-4.mol | [Molecular Weight]
478.54 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [IC 50]
CDK4: 7 nM (IC50) | [References]
[1] Li X, et al. Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors. Bioorg Chem. 2022;121:105669. DOI:10.1016/j.bioorg.2022.105669 |
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