AMG 337
目录号 : GC15655
A selective c-Met inhibitor
Cas No.:1173699-31-4
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
IC50: < 5 nM in enzymatic assays
AMG 337 is a MET inhibitor.
MET receptor with its ligand can promote cell survival, proliferation, and invasion. The activation of MET signaling is a common regulator of various human cancer types, and thus, inhibition of MET signaling is an promising therapeutic opportunity for the treatment of cancer.
In vitro: AMG 337 could effectively inhibit MET kinase activity, and AMG 337 also showed great selectivity for MET when tested against a panel of over 400 protein as well as lipid kinases. In addition, AMG 337 was found to inhibit HGF-dependent MET phosphorylation. Furthermore, AMG 337 could only affect the viability of two gastric cancer cell lines with amplification of the MET gene. The IC50 values of AMG 337 for the two sensitive cell lines was less than 50 nM, whereas over 10 μM in all other tested cell lines [1].
In vivo: In anima study, it was found that the oral administration of AMG 337 led to the dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, which was quite consistent with the PD modulation of MET signaling [1].
Clinical trial: A phase 1 clinical study is currently investigating the safety, tolerability and PK of AMG 337 in patients with solid tumors [2].
References:
[1] Paul E. Hughes, et al. AMG 337, a novel, potent and selective MET kinase inhibitor, has robust growth inhibitory activity in MET-dependent cancer models. Cancer Res October 1, 2014 74; 728
[2] https://clinicaltrials. gov/ct2/show/NCT01253707 term=AMG+337&rank=1
| Cas No. | 1173699-31-4 | SDF | |
| 化学名 | (R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one | ||
| Canonical SMILES | CN1N=CC(C2=CN3C([C@@H](C)N4C=CC(N=CC(OCCOC)=C5)=C5C4=O)=NN=C3C(F)=C2)=C1 | ||
| 分子式 | C23H22FN7O3 | 分子量 | 463.46 |
| 溶解度 | ≥ 46.3mg/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 | 2.1577 mL | 10.7884 mL | 21.5768 mL |
| 5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL |
| 10 mM | 0.2158 mL | 1.0788 mL | 2.1577 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。