ChemicalBook > CAS DataBase List > AMG 458

AMG 458

Product Name: AMG 458
CAS No.: 913376-83-7
Chemical Name: AMG 458
Synonyms: CS-530;AMG 458;AMG458/AMG-458;AMG-458 ，S2747;AMG 458 USP/EP/BP;AMG-458（913376-83-7）;AMG-458, 10 mM in DMSO;AMG-458 AMG458 c-MET inhibitor;AMG458,inhibit,Inhibitor,c-Met/HGFR,AMG-458;1-(2-Hydroxy-2-methylpropyl)-N-[5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl]-5-methyl-3-oxo-2-
CBNumber: CB62500951
Molecular Formula: C30H29N5O5
Formula Weight: 539.58
MOL File: 913376-83-7.mol

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AMG 458 Property

Density: 1.339
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
color: Off-white to pink

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC

Product number: A614415
Product name: AMG-458
Packaging: 10mg
Price: $415
Updated: 2021/12/16

ApexBio Technology

Product number: A8361
Product name: AMG-458
Packaging: 10mg
Price: $478
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: KIN0000398
Product name: AMG-458
Purity: 95.00%
Packaging: 5MG
Price: $505.77
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FA64937
Product name: AMG 458
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Updated: 2021/12/16

Biosynth Carbosynth

Product number: FA64937
Product name: AMG 458
Packaging: 25mg
Price: $700
Updated: 2021/12/16

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AMG 458 Chemical Properties,Usage,Production

Uses

AMG-458 is a potent inhibitor of c-Met with an IC50 of 60 nM.

Biological Activity

amg-458 is a potent and selective inhibitor of human and mouse c-met with ic50 value of 1.2 nm and 2.0 nm respectively.c-met, also known as hepatocyte growth factor receptor, is a receptor tyrosine kinase that can be activated by hepatocyte growth factor/scatter factor (hgf/sf). it is a membrane protein which plays an essential role in embryonic development and wound healing.recent study investigated the effect of amg-456 treatment on cell radiosensitizing response. the results showed that amg-458 treatment enhanced radiosensitivity in h441 with higher levels of c-met but not in a549 with lower expression of c-met [1].this component was also used in an animal model to study the role of c-met in the development of tumor. for instance, orally administration of amg-456 resulted in significant inhibition of tumor growth in /tpr-met and u-87 mg xenograft models without any adverse effect on body weight [2].

in vivo

AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight^[1].

Animal Model:	NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model^[1].
Dosage:	10, 30, 100 mg/kg.
Administration:	Orally q.d. or b.i.d.
Result:	With an ED₅₀ of ～12 mg/kg and an ED₉₀ of ～ 34 mg/kg in NIH-3T3/TPR-Met model. With an ED₅₀ of ～16 mg/kg and an ED₉₀ of ～ 59 mg/kg in U-87 MG human glioblastoma xenograft model. Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.

Animal Model:	Balb/c mouse and SD rat^[1].
Dosage:	1 mg/kg (Pharmacokinetic Analysis).
Administration:	IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
Result:	Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, V_ss (L/kg) values of 0.31 and 0.62, t_1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.

Enzyme inhibitor

This potent c-Met protein kinase inhibitor (FW = 539.58 g/mol; CAS 913376-83-7; Solubility: 21 mg/mL DMSO; ~1 mg/mL H2O), also named 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, targets the MET proto-oncogene product c-Met, which is the hepatocyte growth factor receptor possessing tyrosine-kinase activity. The primary single-chain precursor protein is posttranslationally cleaved to produce the a and b subunits that are disulfide linked to form the mature receptor. Various mutations in the MET gene are associated with papillary renal carcinoma. AMG-458 preferentially inhibits c-Met (Ki = 1.2 nM), showing ~350-fold greater potency than VEGFR2 in cells. AMG-458 significantly inhibited tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight. AMG 458 binds covalently to liver microsomal proteins from rats and humans, even in the absence of NADPH. When [14C]AMG-458 is incubated with liver microsomes in the presence of glutathione or N-acetyl cysteine, quinolone-type thioether adducts can be detected by radiochromatographyand LC/MS/MS analysis. AMG-458 was more effective in cells that expressed higher levels of c-Met/p-Met, suggesting that higher levels of c- Met and p-Met in non-small cell lung cancer (NSCLC) tissue may classify a subset of tumors that are more sensitive to molecular therapies against this receptor.

target

c-Met (H1094R)

IC 50

VEGDR2: 4100 nM (Ki)

References

1. li b, torossian a, sun y, du r, dicker ap, lu b. higher levels of c-met expression and phosphorylation identify cell lines with increased sensitivity to amg-458, a novel selective c-met inhibitor with radiosensitizing effects. int j radiat oncol biol phys 2012,84:e525-531.2. liu l, siegmund a, xi n, kaplan-lefko p, rex k, chen a, 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-meth yl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide (amg 458). j med chem 2008,51:3688-3691.

AMG 458 Preparation Products And Raw materials

Raw materials

Preparation Products

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913376-83-7, AMG 458Related Search:

Capmatinib Selumetinib PHA-665752 PD 0325901 SL 327 Crizotinib

AMG 458

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

1-(2-Hydroxy-2-methylpropyl)-N-[5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl]-5-methyl-3-oxo-2-

CS-530

1H-Pyrazole-4-carboxamide, 2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-N-[5-[(7-methoxy-4-quinolinyl)oxy]-2-pyridinyl]-5-methyl-3-oxo-2-phenyl-

AMG 458 USP/EP/BP

AMG-458 AMG458 c-MET inhibitor

AMG458,inhibit,Inhibitor,c-Met/HGFR,AMG-458

AMG458/AMG-458

AMG-458, 10 mM in DMSO

AMG-458（913376-83-7）

AMG-458 ，S2747

913376-83-7

Inhibitors