AMG-208
CAS No. : 1002304-34-8
| Size | Price | Stock |
|---|---|---|
| 5mg | $65 | In-stock |
| 10mg | $104 | In-stock |
| 25mg | $190 | In-stock |
| 50mg | $300 | In-stock |
| 100mg | $460 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-12035 |
| M.Wt: | 383.40 |
| Formula: | C22H17N5O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 3.33 mg/mL (ultrasonic) |
AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity[1][2][3].
In Vitro: AMG-208 (compound 4) 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 (compound 1) 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].
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[1].
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