tepotinib-emd-1214063

Description: This product has been discontinued. Tepotinib (formerly EMD 1214063, EMD-1214063; MSC2156119; MSC-2156119) is a selective c-Met inhibitor with potential antineoplastic activity. It inhibits c-Met with an IC50 of 4 nM, and is > 200-fold selective for inhibiting c-Met over other kinases such as IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib can inhibit HGF-induced c-Met phosphorylation with an average IC50 of 6 nM in A549 cells. It also significantly inhibits the activation of downstream signaling pathways of c-Met including the phosphorylation of Akt, Gab-1and Erk1/2.

References: Clin Cancer Res. 2013 Jun 1; 19(11):2941-51.

IUPAC/Chemical Name: 3-(1-(3-(5-((1-methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-1, 6-dihydro-6-oxopyridazin-3-yl)benzonitrile

InChi Key: AHYMHWXQRWRBKT-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H28N6O2/c1-34-12-10-21(11-13-34)20-37-26-17-31-29(32-18-26)25-7-3-5-23(15-25)19-35-28(36)9-8-27(33-35)24-6-2-4-22(14-24)16-30/h2-9, 14-15, 17-18, 21H, 10-13, 19-20H2, 1H3

SMILES Code: N#CC1=CC=CC(C(C=C2)=NN(CC3=CC=CC(C4=NC=C(OCC5CCN(C)CC5)C=N4)=C3)C2=O)=C1