AMG-208
目录号 : GC12600
A potent c-Met inhibitor
Cas No.:1002304-34-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 1002304-34-8 | SDF | |
| 化学名 | 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline | ||
| Canonical SMILES | COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5 | ||
| 分子式 | C22H17N5O2 | 分子量 | 383.4 |
| 溶解度 | ≥ 3.83mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。