| 產(chǎn)品描述： | 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 |
| 靶點(diǎn)： |
CYP3A4:32 μM (IC50);c-Met:9 nM (IC50);P450;c-Met/HGFR |
| 體內(nèi)研究： |
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 |
| 參考文獻(xiàn)： |
1. Albrecht BK, 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. 2. Boezio AA, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett. 2009, 19(22), 6307-6312. 3. Liu X, et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol Med. 2010,16(1), 37-45. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.608 ml |
13.041 ml |
26.082 ml |
| 5 mM |
0.522 ml |
2.608 ml |
5.216 ml |
| 10 mM |
0.261 ml |
1.304 ml |
2.608 ml |
| 50 mM |
0.052 ml |
0.261 ml |
0.522 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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