Art. -Nr.: HY-18696

AMG-337

3 Cited Publications

Kundenbewertung

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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Reinheit: 99.40%
CAS. Nr.: 1173699-31-4
Formel: C₂₃H₂₂FN₇O₃
Molecular Weight:463.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AMG-337 Chemical Structure

CAS. Nr.: 1173699-31-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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]

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	5 nM Compound: 23; AMG 337	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	[PMID: 26812066]

In Vitro

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.

Apoptosis Analysis^[1]

Cell Line:

MKN-45 and SNU-620 cells
Concentration:

0, 3, 10, 30, 100 and 300 nM
Incubation Time:

24 hours
Result:

Increased the number of cells undergoing apoptosis.

Cell Cycle Analysis^[1]

Cell Line:

MKN-45 and SNU-620 cells
Concentration:

0, 3, 10, 30, 100 and 300 nM
Incubation Time:

24 hours
Result:

Increased in a dose-dependent in cells in the G1 phase and with concurrent reduction of cells in S-phase.

Western Blot Analysis^[1]

Cell Line:

MKN-45, SNU-620, and SNU-5 cells
Concentration:

100 nM
Incubation Time:

2 hours
Result:

Inhibited MET phosphorylation and phosphorylation of downstream effectors.

Western Blot Analysis^[1]

Cell Line:

MKN-45, SNU-620, and SNU-5 cells
Concentration:

100 nM
Incubation Time:

24 hours
Result:

Induced PARP and caspase-3 cleavage in SNU-620 and SNU-5 cells.

In Vivo

AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models^[1].
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.

Animal Model:

Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts^[1]
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)
Administration:

Oral administration; daily, for 28 days
Result:

Inhibited tumor growth in MET-dependent tumor xenograft models.

Animal Model:

Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts^[1]
Dosage:

0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
Administration:

Oral administration; once, for 3 hours
Result:

Inhibited Gab-1 phosphorylation in a dose-dependent manner.

Animal Model:

Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)^[1]
Dosage:

0, 0.3, 1, and 3 mg/kg
Administration:

Oral administration; once, for 3 or 24 hours
Result:

Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1173699-31-4
Appearance Solid
Molecular Weight 463.46
Formel C₂₃H₂₂FN₇O₃
Color White to off-white
SMILES

O=C1C2=C(N=CC(OCCOC)=C2)C=CN1[C@@H](C3=NN=C4C(F)=CC(C5=CN(C)N=C5)=CN43)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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
Preprints

2025 May 30.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AMG-337

3 Cited Publications

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AMG-337

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

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Anti-Lung Cancer Compound Library

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Cancer Stem Cells Compound Library

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Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AMG-337

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-337 Related Classifications

HY-18696 Related Classifications