Cat. No. Name Size Price Add Cart
KI2807EMD-12140635 mg$416
EMD-121406310 mg$676
EMD-121406320 mg$1040
EMD-121406350 mg$1768
EMD-1214063100 mg$2600
EMD-1214063200 mg$3900
EMD-12140631 g$9100

Chemical Characteristic

Product NameEMD-1214063
CAS No.1100598-32-0
Molecular Weight 492.57
FormulaC29H28N6O2
Chemical Name3-[1-[[3-[5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl]phenyl]methyl]-6-oxopyridazin-3-yl]benzonitrile
SmilesC(#N)c1cc(ccc1)c1ccc(=O)n(n1)Cc1cc(ccc1)c1ncc(cn1)OCC1CCN(CC1)C
Chemical Structure

Biological activities

EMD-1214063 is a potent and selective inhibitor of c-Met. The IC50 against c-Met is 4 nM. EMD-1214063 shows >200-times less selective to IRAK4, TrkA, Axl, IRAK1, and Mer than c-Met. In vitro, EMD-1214063 does-dependently inhibits c-Met phosphorylation and downstream signaling. In murine xenograft models, EMD-1214063 induces regression of human tumors, regardless of whether c-Met activation is HGF dependent or independent. In addition, EMD-1214063 also is well tolerated and induces no substantial weight loss after more than 3 weeks of treatment.[1]

References

[1] Bladt F, et al. EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res. 2013, 19(11): 2941-2951.

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