2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR Caspase Apoptosis
  4. AMG-337

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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AMG-337 Chemical Structure

AMG-337 Chemical Structure

CAS No. : 1173699-31-4

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10 mM * 1 mL in DMSO
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10 mg USD 165 In-stock
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Based on 1 publication(s) in Google Scholar

AMG-337 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

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]
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.

AMG-337 Related Antibodies

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
Molecular Weight

463.46

Formula

C23H22FN7O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.43%

SDS (252 KB)

COA (248 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References

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
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AMG-337 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG-3371173699-31-4AMG337AMG 337c-Met/HGFRCaspaseApoptosisphosphorylationcell proliferationMKN-45SNU-620SNU-5 cellsanticancerInhibitorinhibitorinhibit

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