AMG-208C-Met inhibitor,potent and highly selective CAS# 1002304-34-8 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 1002304-34-8 | SDF | Download SDF |
| PubChem ID | 24864821 | Appearance | Powder |
| Formula | C22H17N5O2 | M.Wt | 383.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | AMG 208;UNII-Y2SR66P7VM | ||
| Solubility | DMSO : 7.8 mg/mL (20.34 mM; Need ultrasonic and warming) | ||
| Chemical Name | 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline | ||
| SMILES | COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5 | ||
| Standard InChIKey | HEAIZQNMNCHNFD-UHFFFAOYSA-N | ||
| Standard 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AMG-208 is a potent and highly selective inhibitor of Met with IC50 value of 9.3 nM. | |||||
| Targets | Met | |||||
| IC50 | 9.3 nM | |||||
AMG-208 Dilution Calculator
AMG-208 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL | 52.1648 mL | 65.2061 mL |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | 10.433 mL | 13.0412 mL |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL | 5.2165 mL | 6.5206 mL |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.0433 mL | 1.3041 mL |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.5216 mL | 0.6521 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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AMG-208 is a highly selective c-Met inhibitor with IC50 value of 9.3 nM [1]. c-Met, the receptor tyrosine kinase, and its natural ligand, hepatocyte growth factor (HGFa), are essential for normal embryonic development and are involved in cell proliferation, migration, and invasion [2].
AMG-208 is a selective c-Met inhibitor. Pre-incubation of AMG-208 with human liver microsomes for 30 minutes inhibited CYP3A4 metabolic activity for eightfold with IC50 value of 4.1 μM in a time-dependent way [1]. In PC3 cells, AMG-208 inhibited HGF-mediated c-Met phosphorylation with IC50 value of 46 nM [2].
In male Sprague-Dawley rats, AMG-208 (0.5 mg/kg i.v.) displays a high bioavailability with Cl value of 0.37 L/h/kg, Vss value of 0.38 L/kg and T1/2 value of 1 hour [2]. Deregulation of c-Met has been involved in several human cancers and AMG-208 can inhibit c-Met activity, which would be used for cancer treatment [2].
References:
[1]. Boezio AA, Berry L, Albrecht BK, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Let,. 2009, 19(22): 6307-6312.
[2]. Albrecht BK, Harmange JC, Bauer D, et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem, 2008, 51(10): 2879-2882.
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A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors.[Pubmed:26155941]
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.
