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GSK1120212 (JTP-74057, Trametinib)

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MEK 抑制剂

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产品目录号: A11029

库存状态:中国现货中国现货

产品名 目录号 价格 数量
GSK1120212 5mg A11029-5
¥ 400.00
GSK1120212 10mg A11029-10
¥ 600.00
GSK1120212 50mg A11029-50
¥ 800.00
GSK1120212 100mg A11029-100
¥ 1,200.00
GSK1120212 10mM * 1mL in DMSO A11029-10mM-D
¥ 550.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.

GSK1120212 (JTP-74057, Trametinib)

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顾客使用 Adooq 产品发表的高质量科研文献
Adooq 顾客使用 GSK1120212 (JTP-74057, Trametinib) 发表的文献 (5)
  • Chul Min Park, .et al. Mechanisms for DNA-damaging agent-induced inactivation of ErbB2 and ErbB3 via the ERK and p38 signaling pathways, Oncol Lett, 2018, Feb; 15(2): 1758每1762 PMID: 29434871
  • Sumi T, .et al. Trametinib downregulates survivin expression in RB1-positive KRAS-mutant lung adenocarcinoma cells, Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
  • Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33每46 PMID: 29658609
  • Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
  • Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070

Chemical Information

目录号 A11029
Mechanism of action Inhibitor
分子量 615.4
化学分子式 C26H23FIN5O4
Solubility DMSO
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 871700-17-3
Synonyms GSK-1120212, GSK212, Trametinib
SMILES code CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5
化学名称 N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]acetamide

生物活性

Description
GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.
Targets
MEK1 (Cell-free assay) MEK2 (Cell-free assay)
0.92 nM1.8 nM

溶解性

Solubility (25°C) * In vitro DMSO 100 mg/mL heating (162.49 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 15 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 16.25 mL 81.25 mL 162.5mL
0.5 mM 3.25 mL 16.25 mL 32.5 mL
1 mM 1.62 mL 8.12 mL 16.25 mL
5 mM 0.32 mL 1.62 mL 3.25 mL

*The above data is based on the productmolecular weight 615.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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