AMG-337
Based on 3 publication(s) in Google Scholar
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
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- 純度: 99.40%
- CAS 番号: 1173699-31-4
- 分子式: C23H22FN7O3
- 分子量:463.46
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 AMG-337
MoreCaspase アイソフォーム固有の製品をすべて表示
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生物活性
IC50: 1 (WT MET), 1 (H1094R MET), 4.7 (M1250T MET), 5 (HGF-stimulated pMET (PC3 cells) MET), 21.5 (V1092I MET), 1077 (Y1230H MET) and >4000 nM (D1228H MET)[1]
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Cell Line
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Type | Value | Description | References |
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| PC-3 | IC50 |
5 nM
Compound: 23; AMG 337
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Inhibition of HGF-mediated MET autophosphorylation in human PC3 cells preincubated for 1 hr followed by stimulation with human HGF measured after 10 mins by electrochemiluminescence immunoassay
Inhibition of HGF-mediated MET autophosphorylation in human PC3 cells preincubated for 1 hr followed by stimulation with human HGF measured after 10 mins by electrochemiluminescence immunoassay
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[PMID: 26812066] |
AMG 337 (0-3 μM; 72 h) inhibits proliferation in MET-dependent cancer cell lines[1].
AMG 337 (0-300 nM; 0-24 h; MKN-45, SNU-620, and SNU-5 cells) inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN-45 and SNU-620 cells
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Concentration:0, 3, 10, 30, 100 and 300 nM
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Incubation Time:24 hours
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Result:Increased the number of cells undergoing apoptosis.
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Cell Line:MKN-45 and SNU-620 cells
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Concentration:0, 3, 10, 30, 100 and 300 nM
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Incubation Time:24 hours
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Result:Increased in a dose-dependent in cells in the G1 phase and with concurrent reduction of cells in S-phase.
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Cell Line:MKN-45, SNU-620, and SNU-5 cells
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Concentration:100 nM
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Incubation Time:2 hours
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Result:Inhibited MET phosphorylation and phosphorylation of downstream effectors.
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Cell Line:MKN-45, SNU-620, and SNU-5 cells
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Concentration:100 nM
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Incubation Time:24 hours
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Result:Induced PARP and caspase-3 cleavage in SNU-620 and SNU-5 cells.
AMG 337 (0-3 mg/kg; p.o.; once, for 3 or 24 h) is associated with increased necrosis in the MET-dependent SNU-620 tumor xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts[1]
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Dosage:0, 0.3, and 1 mg/kg (SNU-620 xenograft); 0, 0.3, 1, 3, and 10 mg/kg (SNU-5 xenograft); 0, 3, 10 and 30 mg/kg (U-87 xenograft)
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Administration:Oral administration; daily, for 28 days
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Result:Inhibited tumor growth in MET-dependent tumor xenograft models.
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Animal Model:Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts[1]
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Dosage:0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
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Administration:Oral administration; once, for 3 hours
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Result:Inhibited Gab-1 phosphorylation in a dose-dependent manner.
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Animal Model:Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)[1]
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Dosage:0, 0.3, 1, and 3 mg/kg
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Administration:Oral administration; once, for 3 or 24 hours
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Result:Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1173699-31-4
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性状 Solid
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分子量 463.46
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分子式 C23H22FN7O3
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Color White to off-white
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SMILES
O=C1C2=C(N=CC(OCCOC)=C2)C=CN1[C@@H](C3=NN=C4C(F)=CC(C5=CN(C)N=C5)=CN43)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Pediatr Surg Int
Clinical characteristics and target exploration via scRNA-seq and high-throughput drug screening of FOXO1 fusion positive rhabdomyosarcoma. [Abstract]2025 Nov 15;42(1):12. PMID: 41240117 -
溶剤 & 溶解度
DMSO : 100 mg/mL (215.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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- Français - FR (393 KB)
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- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hughes PE, et, al. In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models. Mol Cancer Ther. 2016 Jul;15(7):1568-79. [Content Brief]
[2]. Du Z, et, al. Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma. Mol Cancer Ther. 2016 Jun;15(6):1227-37. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1577 mL | 10.7884 mL | 21.5768 mL | 53.9421 mL |
| 5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL | 10.7884 mL | |
| 10 mM | 0.2158 mL | 1.0788 mL | 2.1577 mL | 5.3942 mL | |
| 15 mM | 0.1438 mL | 0.7192 mL | 1.4385 mL | 3.5961 mL | |
| 20 mM | 0.1079 mL | 0.5394 mL | 1.0788 mL | 2.6971 mL | |
| 25 mM | 0.0863 mL | 0.4315 mL | 0.8631 mL | 2.1577 mL | |
| 30 mM | 0.0719 mL | 0.3596 mL | 0.7192 mL | 1.7981 mL | |
| 40 mM | 0.0539 mL | 0.2697 mL | 0.5394 mL | 1.3486 mL | |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4315 mL | 1.0788 mL | |
| 60 mM | 0.0360 mL | 0.1798 mL | 0.3596 mL | 0.8990 mL | |
| 80 mM | 0.0270 mL | 0.1349 mL | 0.2697 mL | 0.6743 mL | |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5394 mL |
AMG-337 関連分類
HY-18696 関連分類
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