WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206543
CAS#: 1207293-36-4
Description: BI-847325 is an orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells.
MedKoo Cat#: 206543
Name: BI-847325
CAS#: 1207293-36-4
Chemical Formula: C29H28N4O2
Exact Mass: 464.2212
Molecular Weight: 464.569
Elemental Analysis: C, 74.98; H, 6.08; N, 12.06; O, 6.89
Synonym: BI-847325; BI 847325; BI847325.
IUPAC/Chemical Name: (Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide
InChi Key: FLBNLJLONKAPLR-DQSJHHFOSA-N
InChi Code: InChI=1S/C29H28N4O2/c1-4-30-26(34)17-13-20-12-16-24-25(18-20)32-29(35)27(24)28(22-8-6-5-7-9-22)31-23-14-10-21(11-15-23)19-33(2)3/h5-12,14-16,18,31H,4,19H2,1-3H3,(H,30,34)(H,32,35)/b28-27-
SMILES Code: O=C(NCC)C#CC1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC=CC=C4
1: Schöffski P, Aftimos P, Dumez H, Deleporte A, De Block K, Costermans J,
Billiet M, Meeus MA, Lee C, Schnell D, Goeldner RG, Awada A. A phase I study of
two dosing schedules of oral BI 847325 in patients with advanced solid tumors.
Cancer Chemother Pharmacol. 2016 Jan;77(1):99-108. doi:
10.1007/s00280-015-2914-5. Epub 2015 Dec 9. PubMed PMID: 26650227.
2: Phadke MS, Sini P, Smalley KS. The Novel ATP-Competitive MEK/Aurora Kinase
Inhibitor BI-847325 Overcomes Acquired BRAF Inhibitor Resistance through
Suppression of Mcl-1 and MEK Expression. Mol Cancer Ther. 2015 Jun;14(6):1354-64.
doi: 10.1158/1535-7163.MCT-14-0832. Epub 2015 Apr 14. PubMed PMID: 25873592;
PubMed Central PMCID: PMC4458462.