GSK1120212 (JTP-74057, Trametinib)

Catalog No. A11029

GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。

Product Citations

Nao Yamagishi, .et al. Non-canonical Regulation of EGFR by the Air Pollutant 9,10-Phenanthrenequinone, Biol Pharm Bull, 2022, 45(10):1553-1558 PMID: 36184515
Hayato Mizuta, .et al. Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer, Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
Keisuke Yanagida, .et al. Sphingosine 1-Phosphate Receptor Signaling Establishes AP-1 Gradients to Allow for Retinal Endothelial Cell Specialization, Dev Cell, 2020, 52 (6), 779-793 PMID: 32059774
Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
Kanemaru Y, .et al. Dramatic response of BRAF V600E-mutant epithelioid glioblastoma to combination therapy with BRAF and MEK inhibitor: establishment and xenograft of a cell line to predict clinical efficacy, Acta Neuropathol Commun, 2019, Jul 25;7(1):119 PMID: 31345255
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): 1758-1762 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): 33-46 PMID: 29658609
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Technical details

Catalog Num	A11029
M. Wt	615.4
Formula	C26H23FIN5O4
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	871700-17-3
Synonyms	GSK-1120212, GSK212, Trametinib
SMILES	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

Biological Activity

GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。

Targets

MEK1 (Cell-free assay)	MEK2 (Cell-free assay)
0.92 nM	1.8 nM

Solubility *

In vitro (25°C)	DMSO	Warmed: 19 mg/mL (30.87 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	4% DMSO+corn oil	2 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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	16.25 mL	81.25 mL	162.5 mL
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.