CAS No. : 1002304-34-8

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000077
Molecular Formula:C₂₂H₁₇N₅O₂
Molecular Weight:383.4
IC50:9.3 nM
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Appearance:Solid powder
Purity: > 98%
Cat No:I000077
Cas No:1002304-34-8

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.
IC50 value: 9.3 nM
Target: c-Met
in vitro: 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 [1]. Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation [2]. AMG-208 is identified to be a c-MET and RON dual selective inhibitor [3].
in vivo: In male SpragueDawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour, while AMG-208 (2 mg/kg i.v.) shows a bioavailability with AUC0→∞ of 2517 ng·h/mL and F of 43%, respectively [1].

1:Oncotarget. 2015 Jul 30;6(21):18693-706. 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, PMID: 26155941 PMCID: PMC4621921 DOI: 10.18632/oncotarget.4472
Abstract: 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.TRIAL REGISTRATION: NCT00813384.
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