SKLB4771 (FLT3-IN-1)
(Synonyms: FLT3-?IN-?1) 目录号 : GC33141
SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10?nM.
Cas No.:1370256-78-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10?nM.
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).[1].
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.[1]
[1] Li WW, et al. J Med Chem. 2012 26;55(8):3852-66.
| Cas No. | 1370256-78-2 | SDF | |
| 别名 | FLT3-?IN-?1 | ||
| Canonical SMILES | O=C(NC1=NN=C(SC2=C3C=CC(OCCCN4CCOCC4)=CC3=NC=N2)S1)NC5=CC=C(C)C=C5 | ||
| 分子式 | C25H27N7O3S2 | 分子量 | 537.66 |
| 溶解度 | DMSO : ≥ 47 mg/mL (87.42 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8599 mL | 9.2996 mL | 18.5991 mL |
| 5 mM | 0.372 mL | 1.8599 mL | 3.7198 mL |
| 10 mM | 0.186 mL | 0.93 mL | 1.8599 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。