Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMG-208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 9,500 | |||
2 mg | 在庫あり | ¥ 13,000 | |||
5 mg | 在庫あり | ¥ 22,500 | |||
10 mg | 在庫あり | ¥ 34,000 | |||
25 mg | 在庫あり | ¥ 61,500 | |||
50 mg | 在庫あり | ¥ 102,500 | |||
100 mg | 在庫あり | ¥ 148,500 |
説明 | AMG-208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1. |
ターゲット&IC50 | c-Met:9 nM |
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] Incubation of AMG-208 with rat and human liver microsomes in the presence of NADPH qualitatively yields C6-phenylarene oxidation products as the major metabolites. [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 Sprague?Dawley 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] |
別名 | AMG 208 |
分子量 | 383.4 |
分子式 | C22H17N5O2 |
CAS No. | 1002304-34-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.8 mg/mL (20.34 mM), Sonication and heating are recommended.
You can also refer to dose conversion for different animals. 詳細
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AMG-208 1002304-34-8 Metabolism Tyrosine Kinase/Adaptors c-Met/HGFR P450 inhibit CYPs Cytochrome P450 Inhibitor AMG 208 AMG208 inhibitor