| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S83019-1mg买3赠1 |
99.10% | ￥300.00 |
6 | - | - | - | - |
|
S83019-2mg买3赠1 |
99.10% | ￥450.00 |
6 | - | - | - | - |
|
S83019-5mg买3赠1 |
99.10% | ￥720.00 |
8 | - | - | - | - |
|
S83019-10mg促销 |
99.10% | ￥1190.00 ￥952.00 |
8 | - | - | - | - |
|
S83019-25mg促销 |
99.10% | ￥2250.00 ￥1800.00 |
4 | - | - | - | - |
|
S83019-50mg促销 |
≥98% | ￥3800.00 ￥3040.00 |
货期：2-3天 | - | - | - | - |
|
S83019-100mg促销 |
≥98% | ￥6500.00 ￥5200.00 |
货期：2-3天 | - | - | - | - |
|
| 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 | ||||||||||||||||||||
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| 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： |
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| 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。 |
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营业执照(三证合一)
北京