A selective c-Met inhibitor
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AMG 337

Item No. 21333

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(1R)-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
CAS Number
1173699-31-4
Molecular Formula
C23H22FN7O3
Formula Weight
463.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mLEthanol: 10 mg/mL
λmax
209, 249, 285, 344 nm
SMILES
COCCOC1=CN=C(C=CN([C@H](C)C2=NN=C3N2C=C(C4=CN(C)N=C4)C=C3F)C5=O)C5=C1
InChi Code
InChI=1S/C23H22FN7O3/c1-14(30-5-4-20-18(23(30)32)9-17(11-25-20)34-7-6-33-3)21-27-28-22-19(24)8-15(13-31(21)22)16-10-26-29(2)12-16/h4-5,8-14H,6-7H2,1-3H3/t14-/m1/s1
InChi Key
DWHXUGDWKAIASB-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

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    10 mg

    $268

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    25 mg

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    Product Description

    AMG 337 is an orally active and selective inhibitor of c-Met kinase activity (IC50 = 1 nM) and adaptor protein Gab-1 phosphorylation, which subsequently blocks downstream PI3K and MAPK pathways.1 It has been shown to inhibit hepatocyte growth factor-mediated c-Met phosphorylation in PC3 cells (IC50 = 5 nM) and to block tumor growth in a c-Met-dependent xenograft model in mice (ED50 = 0.3 mg/kg).1 AMG 337 has been used to inhibit cell proliferation in various c-Met-dependent tumor models.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Boezio, A.A., Copeland, K.W., Rex, K., et al. Discovery of (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 (AMG 337), a potent and selective inhibitor of MET with high unbound target coverage and robust in vivo antitumor activity. J. Med. Chem. 59(6), 2328-2342 (2016).

    2. Hughes, P.E., Rex, K., Caenepeel, S., 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. 15(7), 1568-1579 (2016).

    3. Caenepeel, S., Cooke, K., Wadsworth, S., et al. MAPK pathway inhibition induces MET and GAB1 levels, priming BRAF mutant melanoma for rescue by hepatocyte growth factor. Oncotarget Epub ahead of print, (2017).