T 5601640
(Synonyms: T5601640) 目录号 : GC16355
An inhibitor of LIMK2
Cas No.:924473-59-6
Sample solution is provided at 25 µL, 10mM.
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T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.
T56-LIMKi efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC50 values of 18.3, 7.4, 35.2 and 90 μM, respectively. T56-LIMKi decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma[1]. It blocks the phosphorylation of cofilin which leads to actin severance and inhibition of tumor cell migration, tumor cell growth, and anchorage-independent colony formation in soft agar. T56-LIMKi (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1−/−MEFs with an IC50 of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50μM T56-LIMKi causes a statistically significant reduction in the number of cells exhibiting stress fibers[2].
T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[1].
References:
[1]. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014.
[2]. Mashiach-Farkash E, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.
Cell experiment: | T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[1]. |
Animal experiment: | Mice: T56-LIMKi is dissolved in 0.5% carboxymethylcellulose solution. Mice are implanted with xenografted Panc-1 cells. Treatment is started 7 days later. Mice in the two experimental groups are each treated with a daily oral non-toxic dose of T56-LIMKi (30 or 60 mg/kg in gavage) and mice in the control group receives only the vehicle (0.5% CMC) in the gavage[1]. |
References: [1]. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014. | |
| Cas No. | 924473-59-6 | SDF | |
| 别名 | T5601640 | ||
| 化学名 | 3-methyl-N-(3-((3-(trifluoromethyl)phenyl)carbamoyl)phenyl)isoxazole-5-carboxamide | ||
| Canonical SMILES | O=C(C1=CC=CC(NC(C2=CC(C)=NO2)=O)=C1)NC3=CC(C(F)(F)F)=CC=C3 | ||
| 分子式 | C19H14F3N3O3 | 分子量 | 389.33 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 20 mg/ml | 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 | 2.5685 mL | 12.8426 mL | 25.6852 mL |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.137 mL |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 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。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet