An inhibitor of A-Raf

LY3009120 – 50 mg

Brand:
Cayman
CAS:
1454682-72-4
Storage:
-20
UN-No:
De Minimis - 3077 / 9

LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}  

 

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Description

An inhibitor of A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates); inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays); induces Raf dimerization and inhibits kinase activity of induced dimers

Formal name: N-(3,3-dimethylbutyl)-N’-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]-urea

Synonyms:  DP-4978

Molecular weight: 424.5

CAS: 1454682-72-4

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 Cycle||Research Area|Cancer|Cell Signaling

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