Product Name :
AMG-458
Description:
AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.
CAS:
913376-83-7
Molecular Weight:
539.58
Formula:
C30H29N5O5
Chemical Name:
1-(2-hydroxy-2-methylpropyl)-N-5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide
Smiles :
CC1=C(C(=O)N(C2C=CC=CC=2)N1CC(C)(C)O)C(=O)NC1C=CC(=CN=1)OC1C=CN=C2C=C(C=CC2=1)OC
InChiKey:
GLBZSOQDAOLMGC-UHFFFAOYSA-N
InChi :
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.|Product information|CAS Number: 913376-83-7|Molecular Weight: 539.IL-6 Protein, Human Autophagy 58|Formula: C30H29N5O5|Chemical Name: 1-(2-hydroxy-2-methylpropyl)-N-5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide|Smiles: CC1=C(C(=O)N(C2C=CC=CC=2)N1CC(C)(C)O)C(=O)NC1C=CC(=CN=1)OC1C=CN=C2C=C(C=CC2=1)OC|InChiKey: GLBZSOQDAOLMGC-UHFFFAOYSA-N|InChi: 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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO: 21 mg/mL (38.91 mM)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|AMG 458 also inhibits HGF-mediated c-Met phosphorylation in PC3 and CT26 cells with IC50 of 60 and 120 nM. AMG 458 is observed to bind covalently to liver microsomal proteins from rats and humans in the absence of NADPH.Drotaverine supplier AMG 458 is believed to react with thiol groups in proteins, producing a methoxy quinoline thioether conjugate.PMID:33219878 A recent study shows that the constitutive phosphorylation of c-Met in H441 is abrogated by AMG 458. The basal and HGF-induced phosphorylation of c-Met in A549 is attenuated by AMG 458. The combination of radiation therapy and AMG 458 treatment is found to synergistically increase apoptosis in the H441 cell line by reduction of p-Akt and p-Erk levels, but not in A549.|In Vivo:|AMG 458 is metabolically stable in the liver microsomes of mouse, rat, dog, monkey, and human with low intrinsic clearances (Clint: References:|Liu L, et al. J Med Chem, 2008, 51(13), 3688-3691.Teffera Y, et al. Chem Res Toxicol, 2008, 21(11), 2216-2222.Torossian A, et al. Int J Radiat Oncol Biol Phys, 2012, 84(4), e525-531.Products are for research use only. Not for human use.|