A dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56

Ro 5126766 – 1 mg

Brand:
Cayman
CAS:
946128-88-7
Storage:
-20
UN-No:
- 3077 / 9

Ro 5126766 is a dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45986} It is selective for these kinases over a panel of 254 additional kinases at 10 µM. Ro 5126766 (1 µM) decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM. It inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 65, 28, 40, 46, and 277 nM, respectively) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all).{45987} Oral administration of Ro 5126766 (25 mg/kg four times per day) reduces tumor growth in an HCT116 mouse xenograft model.{45986}  

 

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SKU: 29197 - 1 mg Category:

Description

A dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively); selective for these kinases over a panel of 254 additional kinases at 10 µM; decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM; inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 28-227 nM) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all); reduces tumor growth in an HCT116 mouse xenograft model at 25 mg/kg four times per day

Formal name: N-[3-fluoro-4-[[4-methyl-2-oxo-7-(2-pyrimidinyloxy)-2H-1-benzopyran-3-yl]methyl]-2-pyridinyl]-N′-methyl-sulfamide

Synonyms:  CH5126766

Molecular weight: 471.5

CAS: 946128-88-7

Purity: ≥98%

Formulation: A crystalline solid

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