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

AMG-337 

Cat. No.: HY-18696 Purity: 99.36%
Handling Instructions

AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.

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  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays. IC50 value: < 5nM [1] Target: MET in vitro: AMG-337 demonstrates exquisite selectivity for MET when profiled against a diverse panel of over 400 protein and lipid kinases in a competitive binding assay. In cellular assays, AMG 337 inhibits HGF-dependent MET phosphorylation with an IC50 of < 10 nM. [1] AMG 337 is a selective inhibitor of Met, which inhibits multiple mechanisms of Met activation. [2] in vivo: AMG-337 demonstrates robust activity in MET-dependent cancer models. Oral administration of AMG 337 results in robust dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, with inhibition of tumor growth consistent with the pharmacodynamic modulation of MET signaling.[1]

Clinical Trial
Molecular Weight

463.46

Formula

C₂₃H₂₂FN₇O₃

CAS No.

1173699-31-4

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 provided by MCE.
References

Purity: 99.36%

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Keywords:

AMG-337AMG337AMG 337c-Met/HGFRInhibitorinhibitorinhibit

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Product Name:
AMG-337
Cat. No.:
HY-18696
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