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编 号:F760095
分子式:C26H36N8O
分子量:476.62
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生物活性:
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).

体内研究:
FLT3-IN-18 (10 mg/kg; i.p.; once) 有效抑制大鼠的 FLT3 和 STAT5 磷酸化。Animal Model:Rats (MV4-11 xenografts)
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.

体外研究:
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。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。
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