• 提示：详情请下载说明书。

• 产品描述： SKLB4771是一种有效、选择性的人类受体型酪氨酸蛋白激酶FLT3抑制剂，IC50为10 nM

• 靶点： FLT3(Cell-free assay):10 nM;FLT

• 体外研究：
  SKLB4771 just weakly inhibits Aurora A, FMS, FLT4, and c-Kit (IC50s: 1.5 μM, 2.8 μM, 3.7 μM, and 6.8 μM, respectively). SKLB4771 displays almost no inhibitory activity against the other 13 selected protein kinases. SKLB4771 potently inhibits the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. SKLB4771 just exhibits 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)

• 体内研究：
  Treatment with SKLB4771 at 100 mg/ kg/d results in rapid and complete tumor regression in all mice of this group in the MV4-11 xenograft model. SKLB4771 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slows 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 are observed for all of the SKLB4771-treated mice. The tumor tissues from the SKLB4771-treated groups show significantly fewer Ki67(tumor mitotic index)-positive cells. The TUNEL data shows an obvious increase in the percentage of apoptotic cells in a time-dependent manner.

• 细胞实验： Cell lines: MV4−11, K562, U937, Jurkat, Ramos, Karpas299, HCC827, A549, H2228, H820, PC-9, H292, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, SH-SY5Y Concentrations: increasing concentrations Incubation Time: 72 h Method: The leukemia cells are seeded in a 96-well plate at 1−4 × 104 cells per well, and an equal volume of medium containing increasing concentrations of inhibitors is added to each well. At the end of the incubation period (72 h at 37 °C), 20 μL of 5 mg/mL MTT reagent is added per well for 2−4 h of incubation, and 50 μL of 20% acidified SDS per well is used to lyse the cells. The other cell lines are seeded in 96-well plates at a density of 2−5 × 103 cells/well for 24 h followed by replacement of the medium with serial dilutions of inhibitors in culture medium. Following a 72-h incubation, the MTT reagent is added for a 2−4-h incubation, and 100% DMSO is used to dissolve the cells.

• 动物实验： Animal Models: female NOD-SCID mouse (6−7 weeks old) Dosages: 20 mg/kg, 40 mg/kg, 100 mg/kg Administration: IV

• 参考文献：
  1. Li WW, et al. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 26;55(8):3852-66.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.86 ml	9.3 ml	18.599 ml
  5 mM	0.372 ml	1.86 ml	3.72 ml
  10 mM	0.186 ml	0.93 ml	1.86 ml
  50 mM	0.037 ml	0.186 ml	0.372 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

输入产品批号：

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *