| Identification | Back Directory | [Name]
9H-Purine-2,6-diamine, N2-(trans-4-aminocyclohexyl)-9-cyclopentyl-N6-[4-(4-morpholinyl)phenyl]- | [CAS]
752191-77-8 | [Synonyms]
FLT3-IN-18
9H-Purine-2,6-diamine, N2-(trans-4-aminocyclohexyl)-9-cyclopentyl-N6-[4-(4-morpholinyl)phenyl]- | [Molecular Formula]
C26H36N8O | [MOL File]
752191-77-8.mol | [Molecular Weight]
476.63 |
| Hazard Information | Back Directory | [Uses]
FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML)[1]. | [in vivo]
FLT3-IN-18 (10 mg/kg; i.p.; once) effectively inhibits FLT3 and STAT5 phosphorylation in rats[1]. | Animal Model: | Rats (MV4-11 xenografts)[1] | | Dosage: | 10 mg/kg | | Administration: | I.p.; once | | Result: | Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts, reduced STAT5 phosphorylation by over 95% after 24 h. |
| [References]
[1] Gucky T, et al. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869. DOI:10.1021/acs.jmedchem.7b01529 |
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