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AMG 337

Catalog No.GC15655

AMG 337 est un puissant inhibiteur sélectif de la kinase MET, actif par voie orale, avec des valeurs IC50 de 1, 1, 4,7, 5, 21,5, 1077 et\u003e 4000 nM de WT MET, H1094R MET, M1250T MET, pMET stimulé par HGF (cellules PC3) MET, V1092I MET, Y1230H MET et D1228H MET, respectivement. AMG 337 inhibe la phosphorylation de MET et des effecteurs en aval dans les lignées cellulaires cancéreuses amplifiées par MET, entraînant une inhibition de la prolifération cellulaire dépendante de MET et l'induction de l'apoptose.

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AMG 337 Chemical Structure

Cas No.: 1173699-31-4

Taille Prix Stock Qté
5mg
60,00 $US
En stock
25mg
225,00 $US
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: < 5 nM in enzymatic assays

AMG 337 is a MET inhibitor.

MET receptor with its ligand can promote cell survival, proliferation, and invasion. The activation of MET signaling is a common regulator of various human cancer types, and thus, inhibition of MET signaling is an promising therapeutic opportunity for the treatment of cancer.

In vitro: AMG 337 could effectively inhibit MET kinase activity, and AMG 337 also showed great selectivity for MET when tested against a panel of over 400 protein as well as lipid kinases. In addition, AMG 337 was found to inhibit HGF-dependent MET phosphorylation. Furthermore, AMG 337 could only affect the viability of two gastric cancer cell lines with amplification of the MET gene. The IC50 values of AMG 337 for the two sensitive cell lines was less than 50 nM, whereas over 10 μM in all other tested cell lines [1].

In vivo: In anima study, it was found that the oral administration of AMG 337 led to the dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, which was quite consistent with the PD modulation of MET signaling [1].

Clinical trial: A phase 1 clinical study is currently investigating the safety, tolerability and PK of AMG 337 in patients with solid tumors [2].

References:
[1] Paul E.  Hughes, et al. AMG 337, a novel, potent and selective MET kinase inhibitor, has robust growth inhibitory activity in MET-dependent cancer models. Cancer Res October 1, 2014 74; 728
[2] https://clinicaltrials. gov/ct2/show/NCT01253707 term=AMG+337&rank=1

Chemical Properties

Cas No. 1173699-31-4 SDF
Chemical Name (R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one
Canonical SMILES CN1N=CC(C2=CN3C([C@@H](C)N4C=CC(N=CC(OCCOC)=C5)=C5C4=O)=NN=C3C(F)=C2)=C1
Formula C23H22FN7O3 M.Wt 463.46
Solubility ≥ 46.3mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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