A MEK inhibitor (IC50 = 5 nM); selective for MEK over 400 kinases at 10 µM; inhibits proliferation of COLO 205

RO4987655 – 10 mg

Brand:
Cayman
CAS:
874101-00-5
Storage:
-20
UN-No:
Non-Hazardous - /

RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.  

 

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Description

A MEK inhibitor (IC50 = 5 nM); selective for MEK over 400 kinases at 10 µM; inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells (IC50s = 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively); reduces tumor growth in a variety of mouse xenograft models; inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model at 6.25 mg/kg per day; acts synergistically with everolimus to reduce tumor volume in an HCT116 mouse xenograft model

Formal name: 3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-5-[(tetrahydro-3-oxo-2H-1,2-oxazin-2-yl)methyl]-benzamide

Synonyms:  CH4987655

Molecular weight: 565.3

CAS: 874101-00-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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