| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H17N5O2 |
| Molecular Weight | 383.4027 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(C=C1)C(OCC3=NN=C4C=CC(=NN34)C5=CC=CC=C5)=CC=N2
InChI
InChIKey=HEAIZQNMNCHNFD-UHFFFAOYSA-N
InChI=1S/C22H17N5O2/c1-28-16-7-8-17-19(13-16)23-12-11-20(17)29-14-22-25-24-21-10-9-18(26-27(21)22)15-5-3-2-4-6-15/h2-13H,14H2,1H3
| Molecular Formula | C22H17N5O2 |
| Molecular Weight | 383.4027 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Amgen was developing AMG-208, a small molecule inhibitor of c-Met, for the treatment of cancer. AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. AMG-208 showed evidence of antitumor activity, particularly in prostate cancer. On December 1, 2014 Amgen completed a phase I trial in solid tumours.
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
Three to nine patients were enrolled into one of seven AMG-208 dose cohorts (25, 50, 100, 150, 200, 300, and 400 mg). Patients received AMG-208 orally on days 1 and days 4-28 once daily.
Route of Administration:
Oral
