产品
编 号:F754091
分子式:C25H24N6O2S
分子量:472.56
产品类型
结构图
CAS No: 2620551-45-1
联系客服
产品详情
生物活性:
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model.
体内研究:
FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity.Animal Model:NOD/SCID female mice (subcutaneously implanted MV4-11)
Dosage:1.0 and 3.0 mg/kg
Administration:IP; daily for 28 days
Result:Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.
体外研究:
FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM.FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes.FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner.FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines.FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3.