Chemical Name: N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide. Alternate Names: GSK1120212, JTP-74057
MEK inhibitor
Molecular Weight:
615.39
Purity:
98% by TLC/HPLC NMR (Conforms)
Form:
White solid
CAS Number:
[871700-17-3]
Formula:
C26H23FIN5O4
Application Notes:
Trametinib is a highly potent (IC50 uMEK1 = 0.7 nM, pp-MEK1 = 14.9 nM)1 and selective MEK inhibitor displaying selective inhibition of proliferation in various BRAF mutant cancer cell lines (IC50 ACHN = 9.8 nM, IC50 HT-29 = 0.57 nM)2. It is approved for use against unresectable or metastatic BRAF-mutant melanoma alone or in combination with Dabrafenib. Trametinib can limit outgrowth of tumors without directly inhibiting tumor cell proliferation via abrogation of cytokine-driven expansion of monocytic myeloid-derived suppressor cells (mMDSC) through a mechanism involving CD8+ T cells.3,4 Trametinib also displays potent anti-arthritic effects.5
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