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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > AMG 208CAS：1002304-34-8
Molecular Formula：C22H17N5O2
Molecular Weight：383.4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1002304-34-8 |
| Name | AMG 208 |
| Molecular Formula | C22H17N5O2 |
| Molecular Weight | 383.4 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD17215205 |
| SMILES | COC1=CC=C2C(OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5)=CC=NC2=C1 |
| Target Point | c-Met/HGFR;RON |
| Passage | Protein Tyrosine Kinase/RTK |
| Background | It is a potent, selective dual inhibitor of c-Met/RON and a CYP3A4 inhibitor. |
| Biological Activity | AMG-208 是一种高度选择性的 c-Met 和 RON 的双重抑制剂，对c-Met的IC50值为9 nM。[1] |
| In Vitro | AMG-208 有效抑制激酶c-Met活性，IC50为 9 nM。此外，AMG-208作用于PC3细胞，也抑制HGF调节的 c-Met磷酸化，IC50 为 46 nM。在 NADPH 存在时，AMG-208 和大鼠及人类肝脏微粒温育，造成 C6-phenylarene氧化。[1] AMG-208 与人类肝脏微粒体预温育30分钟，抑制CYP3A4代谢活性，这种作用具有时间依赖性，IC50 为4.1 μM，与没有预温育相比，IC50值降低8倍左右，没有预温育时IC50 为32 μM。[2] AMG-208作为c-MET 和RON双重选择性抑制剂。[3] |
| In Vivo | AMG-208 按0.5 mg/kg剂量粳米粥注射给药雄性Sprague Dawley大鼠，具有显著的生物有效性，Cl为0.37 L/h/kg，Vss 为 0.38 L/kg，T1/2 为1小时，然而AMG-208 按2 mg/kg剂量静脉注射处理，也具有生物有效性，AUC0→∞ 为2517 ng·hour/mL，F为43%。[1] |
| Cell Experiment | Animal Models: 雄性 Sprague-Dawley 大鼠; Dosages: ≤2 mg/kg; Administration: 静脉注射或口服处理[1] |
| Data Literature Source | [1] Albrecht BK，et al. J Med Chem. 2008，51(10)，2879-2882. [2] Boezio AA，et al. Bioorg Med Chem Lett. 2009，19(22)，6307-6312. [3] Liu X，et al. Trends Mol Med. 2010，16(1)，37-45. |
| Unit | Bottle |
| Specification | 5mg 25mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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