纯度:98% by TLC/HPLC;NMR (Conforms)
分子式:C26H23FIN5O4
分子量:615.39
溶剂:DMSO (20 mg/ml, warm)
性状:White solid
存储:-20°C
Activity (short version):MEK inhibitor
Function / Pharmacology: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