An allosteric

Refametinib – 10 mg

Brand:
Cayman
CAS:
923032-37-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Refametinib is an allosteric, selective inhibitor of MEK1 and MEK2 (IC50s = 19 and 47 nM, respectively).{27937} It blocks phosphorylation of ERK1/2 across several human cancer cell lines differing in tissue origin and BRAF mutational status (EC50s = 2.5-16 nM), inhibiting cell cycling in cancer cells but not in primary cells.{27937} Refametinib is orally available and active in human tumor xenograft models.{27937} It has potential utility, particularly in combination therapy, in certain forms of cancer.{27939,27938,27940}  

 

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Description

An allosteric, selective inhibitor of MEK1 and MEK2 (IC50s = 19 and 47 nM, respectively); blocks phosphorylation of ERK1/2 across several human cancer cell lines differing in tissue origin and BRAF mutational status (EC50s = 2.5-16 nM); orally available and active in human tumor xenograft models

Formal name: N-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]-cyclopropanesulfonamide

Synonyms:  ​RDEA119|BAY 86-9766

Molecular weight: 572.3

CAS: 923032-37-5

Purity: ≥95%

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 Cycle||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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