| Bioactivity | 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]. |
| Target | IC50: 0.003 µM (FLT3) |
| Invitro | FLT3-IN-18(compound 7d) (0, 0.01, 0.1, 1, 10, 100 nM; 1h) 在 MV4-11 细胞中呈剂量依赖性降低 p-FLT3 Y589/591，p-FLT3 Y842，p-TAT5 Y694，p-ERK1/2 T202/Y204，p-MEK1/2 S217/221，p-AKT S473 的蛋白表达[1]。FLT3-IN-18 (0, 0.01, 0.1, 1, 10, 100 nM; 24 h) 诱导细胞凋亡和细胞周期停滞在 G1 期[1]。 Cell Proliferation Assay[1] Cell Line: |
| In Vivo | FLT3-IN-18 (10 mg/kg; i.p.; once) 有效抑制大鼠的 FLT3 和 STAT5 磷酸化[1]。 Animal Model: |
| Name | FLT3-IN-18 |
| CAS | 752191-77-8 |
| Formula | C26H36N8O |
| Molar Mass | 476.62 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gucký 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. |