Name: RO4927350
Rating: 5 (10 reviews)

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HIT ID:HIT220912583
Cas No:876755-27-0
常用名:RO4927350
IUPAC:(2S,3S)-2-[(4R)-4-[4-(2-hydroxyethoxy)phenyl]-2,5-dioxoimidazolidin-1-yl]-3-phenyl-N-(4-propanoyl-1,3-thiazol-2-yl)butanamide
IUPAC:(2S,3S)-2-[(4R)-4-[4-(2-hydroxyethoxy)phenyl]-2,5-dioxoimidazolidin-1-yl]-3-phenyl-N-(4-propanoyl-1,3-thiazol-2-yl)butanamide
InChI key:InChIKey=RKKBPPTYPGTSEA-FNVCAUGXSA-N

分子式:C27H28N4O6S
分子量:536.6
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:CCC(=O)c1csc(NC(=O)[C@H]([C@@H](C)c2ccccc2)N2C(=O)N[C@@H](C2=O)c2ccc(OCCO)cc2)n1
SMILES:CCC(=O)c1csc(NC(=O)[C@H]([C@@H](C)c2ccccc2)N2C(=O)N[C@@H](C2=O)c2ccc(OCCO)cc2)n1

RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback increase in MEK phosphorylation, which has been observed with other MEK inhibitors. RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation.

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