| References: |
FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
in vitro: FLT3-IN-1 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. FLT3-IN-1 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt’s lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y.
in vivo: Treatment with FLT3-IN-1 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. FLT3-IN-1 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the FLT3-IN-1-treated mice. For the detailed information of FLT3-IN-1, the solubility of FLT3-IN-1 in water, the solubility of FLT3-IN-1 in DMSO, the solubility of FLT3-IN-1 in PBS buffer, the animal experiment (test) of FLT3-IN-1, the cell expriment (test) of FLT3-IN-1, the in vivo, in vitro and clinical trial test of FLT3-IN-1, the EC50, IC50,and affinity,of FLT3-IN-1, For the detailed information of FLT3-IN-1, the solubility of FLT3-IN-1 in water, the solubility of FLT3-IN-1 in DMSO, the solubility of FLT3-IN-1 in PBS buffer, the animal experiment (test) of FLT3-IN-1, the cell expriment (test) of FLT3-IN-1, the in vivo, in vitro and clinical trial test of FLT3-IN-1, the EC50, IC50,and affinity,of FLT3-IN-1, Please contact DC Chemicals. |
