A selective dual MEK/Aurora kinase inhibitor (IC50s = 3

BI-847325 – 1 mg

Brand:
Cayman
CAS:
1207293-36-4
Storage:
-20
UN-No:
Non-Hazardous - /

BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC50 values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively.{29630} It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim.{29630} At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.{29630}  

 

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Description

A selective dual MEK/Aurora kinase inhibitor (IC50s = 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively); inhibits the growth and survival of both treatment-naïve and drug-resistant melanoma both in vitro and in vivo, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim

Formal name: 3-[3-[[[4-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide

Synonyms: 

Molecular weight: 464.6

CAS: 1207293-36-4

Purity: ≥98%

Formulation: A crystalline solid

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

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