英文别名：946128-88-7|RO5126766|avutometinib|CH5126766|RO-5126766|RO-5126766 free base|Ro 5126766|CH-5126766|RO5126766(CH5126766)|RG-7304|VS-6766|CKI-27|3-[[2-[(methylaminosulfonyl)amino]-3-fluoropyridin-4-yl]methyl]-4-methyl-7-[(pyrimidin-2-yl)oxy]-2H-1-benzopyran

纯度：10mM in DMSO

货号：R427048

Cas号：946128-88-7

存储温度：-80℃储存

产品介绍：

Information

RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304) is a dualRAF/MEKinhibitor withIC50of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.

Targets

BRAF V600E (cell-free assay); BRAF (cell-free assay); CRAF (cell-free assay); MEK1 (cell-free assay) 8.2 nM; 19 nM; 56 nM; 160 nM

In vitro

In HCT116 KRAS-mutant colorectal cancer cells, CH5126766 significantly reduces the levels of phospho-MEK and phospho-ERK. CH5126766 inhibits RAF kinase by binding to MEK1, and causes MEK to become a dominant negative inhibitor of RAF. In Raf or RAS-mutant cell lines SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, HCT116, and PC3 cells, CH5126766 inhibits cell growth with IC50 of 65, 28, 40, 46, and 277 nM, respectively. In two melanoma cell lines with the BRAF V600E or NRAS mutation, RO5126766 induces G1 cell cycle arrest accompanied by up-regulation of the CDK inhibitor p27 and down-regulation of cyclinD1.

In vivo

In an HCT116 (G13D KRAS) mouse xenograft model, CH5126766 (25 mg/kg, p.o.) inhibits ERK signaling output more effectively than a standard MEK inhibitor that induces MEK phosphorylation and has potent antitumor activity. In the HCT116 (K-ras) and COLO205 (B-raf) mutant xenografts, CH5126766 (0.3 mg/kg) causes significant decreases in [18\u2009F]FDG uptake. In the SK-MEL-2 xenograft model, RO5126766 also suppresses the tumor growth.

Cell Research(from reference)

Cell lines：SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, A549, HCT15, HCT116, and PC3 cells

Concentrations：~10 μM

Incubation Time：72 h

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