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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-NFX-179
NFX-179

Chemical Structure : NFX-179

CAS No.: 2252314-46-6

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NFX-179 (Nedometinib, NFX179, NFX 179)

货号: PC-21237Not For Human Use, Lab Use Only.

NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1).

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10 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1).
NFX-179 is specific for MEK1 inhibition and does not have substantial interactions across a panel of more than 150 kinases or a separate panel of 44 targets of particular relevance for neurological or cardiac toxicity.
NFX-179 potently inhibits phosphorylated-ERK (p-ERK) expression in a malignant peripheral nerve sheath tumor cell line HCT116 (KRAS-mutant G13D) and A375 (BRAF-mutant V600E) with IC50 of 164 nM and 12 nM, respectively.
NFX-179 gel (topical application) significantly reduced the formation of new cSCCs in ultraviolet-induced cSCC mouse models.
NFX-179 inhibits the growth of human SCC cell lines in a dose-dependent manner, and topical NFX-179 application penetrates human skin and inhibits MAPK signaling in human cutaneous squamous cell carcinoma (cSCC) explants.

物理化学性质&存储条件

分子量 470.24
分子式 C17H16FIN4O3
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

2-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)-1-methyl-1H-pyrrolo[2,3-b]pyridine-3-carboxamide

参考文献

1. Sarin KY, et al. Sci Transl Med. 2023 Oct 11;15(717):eade1844.

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