A c-Met inhibitor
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AMG 458

Item No. 36213

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-N-[5-[(7-methoxy-4-quinolinyl)oxy]-2-pyridinyl]-5-methyl-3-oxo-2-phenyl-1H-pyrazole-4-carboxamide
CAS Number
913376-83-7
Molecular Formula
C30H29N5O5
Formula Weight
539.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
234, 301 nm
SMILES
O=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=CC=C(C=N3)OC4=CC=NC5=C4C=CC(OC)=C5
InChi Code
InChI=1S/C30H29N5O5/c1-19-27(29(37)35(20-8-6-5-7-9-20)34(19)18-30(2,3)38)28(36)33-26-13-11-22(17-32-26)40-25-14-15-31-24-16-21(39-4)10-12-23(24)25/h5-17,38H,18H2,1-4H3,(H,32,33,36)
InChi Key
GLBZSOQDAOLMGC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    AMG 458 is an inhibitor of c-Met (Kis = 1.2, 1.1, 2.2, 4.1, 0.5, and 4.5 nM for wild-type c-Met, c-MetV1092I, c-MetD1228H, c-MetM1250T, c-MetH1094R, and c-MetY1230H, respectively).1 It inhibits c-Met phosphorylation in PC3 and CT26 cells (IC50s = 60 and 120 nM, respectively). AMG 458 (30 and 100 mg/kg) reduces tumor volume in NIH3T3 and U87MG mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, L., Siegmund, A., Xi, N., et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J. Med. Chem. 51(13), 3688-3691 (2008).