1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. AMG-337

AMG-337 

Cat. No.: HY-18696 Purity: 99.43%
Handling Instructions

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.

For research use only. We do not sell to patients.

AMG-337 Chemical Structure

AMG-337 Chemical Structure

CAS No. : 1173699-31-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 101 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 99 In-stock
Estimated Time of Arrival: December 31
10 mg USD 165 In-stock
Estimated Time of Arrival: December 31
25 mg USD 275 In-stock
Estimated Time of Arrival: December 31
50 mg USD 495 In-stock
Estimated Time of Arrival: December 31
100 mg USD 825 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1375 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 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]

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].

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].

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.
SMILES

O=C1C2=C(N=CC(OCCOC)=C2)C=CN1[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (215.77 mM; Need ultrasonic)

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
10 mM 0.2158 mL 1.0788 mL 2.1577 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.43%

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AMG-337
Cat. No.:
HY-18696
Quantity:
MCE Japan Authorized Agent: