A MEK1 inhibitor (IC50 = 3.2 nM); inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM); inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM

TAK-733 – 5 mg

Brand:
Cayman
CAS:
1035555-63-5
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-733 is an inhibitor of MEK1 (IC50 = 3.2 nM), a MAP kinase in the Raf/MEK/ERK pathway that plays a major role in the regulation of cellular growth, differentiation, and proliferation.{37319},{17156} It is selective for MEK1 over a panel of 18 kinases, receptors, and ion channels up to a concentration of 10 µM. TAK-733 inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM). It also inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC50s = V600E mutations.{37319},{37320} TAK-733 has antitumor activity in mouse xenograft models using a variety of cancer types.{37319}  

 

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Description

A MEK1 inhibitor (IC50 = 3.2 nM); inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM); inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC50s = V600E mutations,

Formal name: 3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-[(2-fluoro-4-iodophenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione

Synonyms: 

Molecular weight: 504.2

CAS: 1035555-63-5

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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