AMG208 - CAS 1002304-34-8
Catalog number: 1002304-34-8
Category: Inhibitor
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Molecular Formula:
C22H17N5O2
Molecular Weight:
383.411
COA:
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Targets:
c-Met/HGFR
Description:
AMG 208 is a selective small-molecule inhibitor of the proto-oncogene c-Met with potential antineoplastic activity. C-Met encodes the hepatocyte growth factor receptor tyrosine kinase, plays an important role in epithelial cell proliferation and has been shown to be overexpressed in a variety of cancers.
Purity:
0.98
Appearance:
White to off-white solid
Synonyms:
AMG-208; AMG208; AMG 208
MSDS:
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InChIKey:
HEAIZQNMNCHNFD-UHFFFAOYSA-N
InChI:
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
Canonical SMILES:
COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5
Current Developer:
Amgen, Inc.
1.A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors.
Hong DS;Rosen P;Lockhart AC;Fu S;Janku F;Kurzrock R;Khan R;Amore B;Caudillo I;Deng H;Hwang YC;Loberg R;Ngarmchamnanrith G;Beaupre DM;Lee P Oncotarget. 2015 Jul 30;6(21):18693-706.
BACKGROUND: ;This first-in-human study evaluated AMG 208, a small-molecule MET inhibitor, in patients with advanced solid tumors.;METHODS: ;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. The primary objectives were to evaluate the safety, tolerability, pharmacokinetics, and maximum tolerated dose (MTD) of AMG 208.;RESULTS: ;Fifty-four patients were enrolled. Six dose-limiting toxicities were observed: grade 3 increased aspartate aminotransferase (200 mg), grade 3 thrombocytopenia (200 mg), grade 4 acute myocardial infarction (300 mg), grade 3 prolonged QT (300 mg), and two cases of grade 3 hypertension (400 mg). The MTD was not reached. The most frequent grade ≥3 treatment-related adverse event was anemia (n = 3) followed by hypertension, prolonged QT, and thrombocytopenia (two patients each). AMG 208 exposure increased linearly with dose; mean plasma half-life estimates were 21.4-68.7 hours. One complete response (prostate cancer) and three partial responses (two in prostate cancer, one in kidney cancer) were observed.;CONCLUSIONS: ;In this study, AMG 208 had manageable toxicities and showed evidence of antitumor activity, particularly in prostate cancer.
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CAS 1002304-34-8 AMG208

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