Trametinib

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP02307CAS No. ：871700-17-3Purity：98%

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CAS No.	871700-17-3	Cat. No.	BCP02307
Name	Trametinib
Synonyms	GSK-1120212;JTP 74057;GSK1120212;GSK 1120212;JTP-74057;JTP74057;
SMILES
Chemical Name
Formula	C26H23FIN5O4	M. Wt	615.39
Purity	98%	Storage	Store at 4-8°C
Description	GSK1120212 inhibits the phosphorylation of MBP regardless of the isotype of Raf and MEK, with IC50 ranging from 0.92 nM to 3.4 nM. GSK1120212 demonstrates no inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. In addition, GSK1120212 does not show drastic inhibitory activity against the other 98 kinases. GSK1120212 displays potent inhibitory activity against human colorectal cancer cell lines. HT-29 and COLO205 cells, which are known to have a constitutively active B-Raf mutant, are most sensitive to GSK1120212 with IC50 0.48 nM and 0.52 nM, respectively. The cell lines bearing a K-Ras mutation show a wide range of sensitivity to GSK1120212 with IC50 of 2.2-174 nM. In contrast, COLO320 DM cells, bearing the wild-type gene in both B-Raf and K-Ras, are found to be resistant to GSK1120212 even at 10 μM. GSK1120212 treatment for 24 hours induces cell-cycle arrest at the G1 phase in all sensitive cell lines. Consistently, GSK1120212 treatment leads to upregulation of p15INK4