A c-Met and Ron inhibitor
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Isomer(s)
25233Ningetinib
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AMG 1

Item No. 41226

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-fluoro-4-[(7-methoxy-4-quinolinyl)oxy]phenyl]-2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-1H-pyrazole-4-carboxamide
CAS Number
913376-84-8
Synonyms
  • KIN001-237
  • KIN237
  • RON-IN-1
  • RON Inhibitor 1
  • SYN1143
Molecular Formula
C31H29FN4O5
Formula Weight
556.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
OC(C)(C)CN(C(C)=C1C(NC2=CC(F)=C(OC3=C(C=CC(OC)=C4)C4=NC=C3)C=C2)=O)N(C5=CC=CC=C5)C1=O
InChi Code
InChI=1S/C31H29FN4O5/c1-19-28(30(38)36(21-8-6-5-7-9-21)35(19)18-31(2,3)39)29(37)34-20-10-13-27(24(32)16-20)41-26-14-15-33-25-17-22(40-4)11-12-23(25)26/h5-17,39H,18H2,1-4H3,(H,34,37)
InChi Key
UYMSIPINLJNNOU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $218

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    25 mg

    $455

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    50 mg

    $666

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    Product Description

    AMG 1 is an inhibitor of c-Met and Ron (IC50s = 4 and 9 nM, respectively).1 It is selective for c-Met and Ron over seven tyrosine and serine/threonine kinases (IC50s = 160 to 1,900 nM). AMG 1 decreases the levels of phosphorylated MET, ERK1/2, and Akt in HT-29 colon and BxPC-3 pancreatic cancer cells, as well as reduces migration in a wound-healing assay using NIH3T3/TPR-Met fibroblasts, in a concentration-dependent manner. It reduces tumor volume in a U87 glioma mouse xenograft model when administered at a dose of 30 mg/kg twice per day. AMG 1 increases bone volume and bone regrowth area in a mouse model of calvarial defect when administered at a dose of 50 µg in an absorbable collagen sponge.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, Y., Kaplan-Lefko, P.J., Rex, K., et al. Identification of a novel recepteur d’origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 68(16), 6680-6687 (2008).

    2. Kim, J.-W., Lee, M.N., Jeong, B.-C., et al. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur. J. Pharmacol. 806, 10-17 (2017).