CEP-37440
目录号 : GC15273
A dual inhibitor of FAK1 and ALK
Cas No.:1391712-60-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 1000 nM for the proliferation in SUM190 cell lines
The focal adhesion kinase FAK1 is a cytoplasmic tyrosine kinase that localizes to focal adhesions, and controls a number of cell pathways including proliferation, viability and survival. Anaplastic lymphoma kinase 1 (ALK-1) is a member of the insulin receptor tyrosine kinase family. ALK mutations have also been implicated in the pathogenesis of non-small cell lung cancer (NSCLC) and other solid tumors. CEP-37440 is a highly selective and potent dual inhibitor of ALK and FAK1.
In vitro: 300 nM CEP-37440 was able to decrease the proliferation of the triple negative FC-IBC02 cell line and, 1000 nM CEP-37440 was able to complete inhibit the proliferation of these cells. Genes involved in functions such as cellular growth and proliferation, cell cycle, cell death and survival and cellular movement and cell-to cell signaling and interaction were differentially regulated by CEP-37440 in sensitive IBC cell lines. Among them, TGFβ1 and MMP3 were down-regulated and DKK3, CAV1 and TFPI2 were up-regulated by CEP-37440, which might be probalby caused by its dual inhibition of ALK and FAK1 [1].
In vivo: In FC-IBC02 orthotopic breast cancer xenograft models, CEP-37440 was able to reduce the growth of the primary tumor and inhibit the development of spontaneous metastases in brain [1].
Clinical trials: CEP-37440 is a dual ALK/FAK inhibitor currently under investigation in a phase I trial to determine its MTD in patients with advanced or metastatic solid tumors (NCT01922752).
Reference:
[1] Abstract 3232: CEP-37440, a highly selective and potent dual inhibitor of ALK and FAK1 inhibits the proliferation of inflammatory breast cancer cells. Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA
| Cas No. | 1391712-60-9 | SDF | |
| 化学名 | (Z)-2-((E)-(5-chloro-2-(((S)-6-(4-(2-hydroxyethyl)piperazin-1-yl)-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)amino)pyrimidin-4(3H)-ylidene)amino)-N-methylbenzimidic acid | ||
| Canonical SMILES | C/N=C(O)/C1=CC=CC=C1/N=C(N2)\C(Cl)=CN=C2NC3=C(OC)C(CCC[C@@](N4CCN(CCO)CC4)([H])C5)=C5C=C3 | ||
| 分子式 | C30H38ClN7O3 | 分子量 | 580.12 |
| 溶解度 | ≥ 9.25mg/mL in DMSO with gentle warming | 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 | 1.7238 mL | 8.6189 mL | 17.2378 mL |
| 5 mM | 0.3448 mL | 1.7238 mL | 3.4476 mL |
| 10 mM | 0.1724 mL | 0.8619 mL | 1.7238 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet