Cobimetinib hemifumarate
(Synonyms: 考比替尼半富马酸盐; GDC-0973 hemifumarate; XL-518 hemifumarate) 目录号 : GC35719
A potent, orally available MEK1 inhibitor
Cas No.:1369665-02-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cobimetinib is a potent, orally available inhibitor of MEK1 (IC50 = 4.2 nM).1,2 It shows more than 100-fold selectivity for MEK when tested against a panel of more than 100 serine-threonine and tyrosine kinases. Cobimetinib induces differentiation and apoptosis in cancer cell lines and is more effective when combined with additional inhibitors, like PLX4032 .2,3,4
1.Akinleye, A., Furgan, M., Mukhi, N., et al.MEK and the inhibitors: From bench to bedsideJ. Hematol. Oncol.627(2013) 2.Hoeflich, K.P., Merchang, M., Orr, C., et al.Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibitionCancer Res.72(1)210-219(2012) 3.Medina, T.M., and Lewis, K.D.The evolution of combined molecular targeted therapies to advance the therapeutic efficacy in melanoma: A highlight of vemurafenib and cobimetinibOnco Targets Ther.93739-3752(2016) 4.Sing, A., Ruan, Y., Tippett, T., et al.Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cellsJ. Exp. Clin. Cancer Res.34(1)104(2015)
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5447 mL | 7.7234 mL | 15.4469 mL |
| 5 mM | 0.3089 mL | 1.5447 mL | 3.0894 mL |
| 10 mM | 0.1545 mL | 0.7723 mL | 1.5447 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。