Trametinib CAS: 871700-17-3
MF: C26H23FIN5O4
MW: 615.39

Trametinib (CAS 871700-17-3)

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別名: Trametinib is also known as GSK1120212.
アプリケーション: Trametinib is an allosteric inhibitor of MEK1/MEK2 that reduces tumor growth in mouse xenograft models.
CAS 番号: 871700-17-3
Purity: ≥98%
Molecular Weight: 615.39
Molecular Formula: C26H23FIN5O4
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* Refer to Certificate of Analysis for lot specific data (including water content).
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Trametinib is an allosteric reversible, selective MEK1/MEK2 kinase activity inhibitor. Trametinib has an IC50 of 0.7 and 0.9 nM for MEK1 and MEK2, respectively. Trametinib is combined with dabrafenib to formulate a solution that can be used in the treatment of metastatic mutant B-RAFV600E melanoma. Trametinib inhibits the growth of two human colorectal cancer cell lines expressing mutant B-RAF. Trametinib also inhibits the growth of seven cell lines expressing mutant K-Ras, but does not inhibit the growth of wild-type COLO 320DM cells expressing both B-RAF and K-Ras.


参考文献

1. Yamaguchi, T., Kakefuda, R., Tajima, N., et al.Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int. J. Oncol. 39(1), 23-31 (2011).
2. Yamaguchi, T., Kakefuda, R., Tanimoto, A., et al.Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: A comparison with leflunomide. Inflamm. Res. 61(5), 445-454 (2012).

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/mL at 25° C), water (<1 mg/mL at 25° C), ethanol (<1 mg/mL at 25° C), and 30% PEG400/0.5% Tween80/5% propylene glycol (15 mg/ml).
保存方法 :
Store at -20° C
Density :
~1.7 g/cm3 (Predicted)
Refractive Index :
n20D 1.73 (Predicted)
IC50 :
MEK1: IC50 = 0.92 nM; MEK2: IC50 = 1.8 nM
pK Values :
pKb: 0.26 (Predicted)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
PubChem CID :
MDL Number :
MFCD17215075
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

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分析表

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Trametinib (CAS 871700-17-3)  参考文献

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引用 1 to 10 of 18 合計

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PMID: # 27301426  Wang, X.|Chow, CR.|Ebine, K.|Lee, J.|Rosner, MR.|Pan, T.|Munshi, HG.| et al. 2016. Sci Rep. 6: 28260.

PMID: # 26324703  Jones, CL. et al. 2015. Blood. 126: 2202-12.

PMID: # 26309093  Chan, IH. et al. 2015. Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research. 35: 948-55.

PMID: # 25615947  Mas, C. et al. 2015. J. Biotechnol. 205: 111-9.

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