Glumetinib
(Synonyms: 谷美替尼,SCC244) 目录号 : GC64947
A potent c-Met inhibitor
Cas No.:1642581-63-2
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
Glumetinib is a potent inhibitor of c-Met (IC50 = 0.42 nM).1 It is greater than 2,400-fold selective for c-Met over a panel of 312 kinases. Glumetinib (0.001-1 μM) inhibits c-Met phosphorylation in and proliferation of MET-overexpressing EBC-1 lung and MKN45 gastric cancer cells. It inhibits NCI H441 cell motility and invasion induced by hepatocyte growth factor (HGF) when used at a concentration of 10 nM. Glumetinib (2.5-10 mg/kg) reduces tumor volume in MKN45, SNU-5, and EBC-1 mouse xenograft models. It also reduces tumor growth in MET amplification-containing non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC) patient-derived xenograft (PDX) mouse models.
1.Ai, J., Chen, Y., Peng, X., et al.Preclinical evaluation of SCC244 (glumetinib), a novel, potent, and highly selective inhibitor of c-Met in MET-dependent cancer modelsMol. Cancer Ther.17(4)751-762(2017)
| Cas No. | 1642581-63-2 | SDF | Download SDF |
| 别名 | 谷美替尼,SCC244 | ||
| 分子式 | C21H17N9O2S | 分子量 | 459.48 |
| 溶解度 | DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic) | 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 | 2.1764 mL | 10.8819 mL | 21.7637 mL |
| 5 mM | 0.4353 mL | 2.1764 mL | 4.3527 mL |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1764 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。
Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models
Mol Cancer Ther 2018 Apr;17(4):751-762.PMID:29237805DOI:10.1158/1535-7163.MCT-17-0368
Because the receptor tyrosine kinase c-Met plays a critical role in tumor growth, metastasis, tumor angiogenesis, and drug resistance, the c-Met axis represents an attractive therapeutic target. Herein, we report the first preclinical characterization of SCC244, a novel, potent, and highly selective inhibitor of c-Met kinase. SCC244 showed subnanomolar potency against c-Met kinase activity and high selectivity versus 312 other tested protein kinases, making it one of the most selective c-Met inhibitors described to date. Moreover, this inhibitor profoundly and specifically inhibits c-Met signal transduction and thereby suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells. In xenografts of human tumor cell lines or non-small cell lung cancer and hepatocellular carcinoma patient-derived tumor tissue driven by MET aberration, SCC244 administration exhibits robust antitumor activity at the well-tolerated doses. In addition, the in vivo antitumor activity of SCC244 involves the inhibition of c-Met downstream signaling via a mechanism of combined antiproliferation and antiangiogenic effects. The results of the current study provide a strong foundation for the clinical investigation of SCC244 in patients with tumors harboring c-Met pathway alterations. Mol Cancer Ther; 17(4); 751-62. ©2017 AACR.