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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-FCN-159
FCN-159

Chemical Structure : FCN-159

CAS No.: 2739690-43-6

FCN-159 (Luvometinib, FCN159)

货号: PC-24957Not For Human Use, Lab Use Only.

FCN-159 (Luvometinib) is an orally available and highly potent selective MEK1/2 inhibitor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FCN-159 (Luvometinib) is an orally available and highly potent selective MEK1/2 inhibitor.
FCN-159 (Luvometinib) is 10 times more selective than trametinib, and blocks downstream MAPK signalling.
FCN-159 (Luvometinib) exhibits remarkable potency against the cell proliferation of a panel of human cancer cell lines with RAS/RAF mutations while sparing normal or cancer cell lines expressing wild type RAS/RAF, indicating highly selective inhibition against RAS/RAF/MEK signaling pathway.
FCN-159 (Luvometinib) dose-dependently inhibits the phosphorylation of MEK downstream effector ERK and induced cell cycle arrest as well as cell apoptosis in human colon cancer cells.
FCN-159 (Luvometinib) shows significant and dose-dependent anti-tumor activities in a variety of human tumor xenograft models, derived from colon cancer (HT-29 and Colo205), melanoma (A375), NSCLC (Calu-6) and AML (HL-60).
FCN-159 (Luvometinib) potently inhibits tumor growth in two patient-derived xenograft (PDX) models bearing NRAS mutation.

物理化学性质&存储条件

分子量 665.45
分子式 C26H22F2IN5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclopropanesulfonamide, N-[3-[6-cyclopropyl-3-fluoro-4-[(2-fluoro-4-iodophenyl)amino]-1,2,5,6-tetrahydro-1-methyl-2,5-dioxopyrido[2,3-d]pyridazin-8-yl]phenyl]-

参考文献

1. Mao L, et al. Eur J Cancer. 2022 Nov;175:125-135.

2. Shu Lin, et al. Cancer Res (2020) 80 (16_Supplement): 1951.

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