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AMG 900

AMG 900 Struktur
945595-80-2
CAS-Nr.
945595-80-2
Englisch Name:
AMG 900
Synonyma:
AMG 900;AMG-900;AMG900;AMG 900 USP/EP/BP;N-(4-((3-(2-Aminopyrimidin-4-yl)pyridin-2-yl)oxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1;N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine;1-Phthalazinamine, N-[4-[[3-(2-amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-;N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine AMG 900
CBNumber:
CB82554079
Summenformel:
C28H21N7OS
Molgewicht:
503.58
MOL-Datei:
945595-80-2.mol

AMG 900 Eigenschaften

Siedepunkt:
778.7±70.0 °C(Predicted)
Dichte
1.380
storage temp. 
2-8°C(protect from light)
L?slichkeit
≥25.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Aggregatzustand
solid
pka
4.79±0.30(Predicted)
Farbe
Light yellow to yellow

Sicherheit

AMG 900 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Their expression is elevated in a variety of human cancers. AMG 900 is an orally bioavailable, selective Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively. It is greater than 10-fold selective for Aurora kinases over p38α, TYK2, JNK2, Met, and Tie2 (IC50s = 53, 220, 520, 550, and 650 nM, respectively). At 2-3 nM, AMG 900 has been shown to inhibit the proliferation of 26 different tumor cell lines in vitro, including cell lines resistant to either the antimitotic agent paclitaxel or to other Aurora kinase inhibitors. Furthermore, AMG 900 is reported to be broadly active in multiple xenograft models, including three multidrug-resistant xenograft models, representing five tumor types.

Enzyminhibitor

This potent and highly selective mitotic protein kinase inhibitor (FW = 503.58 g/mol; CAS 945595-80-2; Solubility: 100 mg/mL DMSO), also named N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4- methylthiophen-2-yl)phthalazin-1-amine, targets Aurora A (IC50 = 5 nM), Aurora B (IC50 = 4 nM), and Aurora C (IC50 = 1 nM) protein kinases, with >10-fold selectivity versus p38α, Tyk2, JNK2, Met and Tie2. The modal tumor cell response to AMG 900 treatment is aborted cell division without prolonged mitotic arrest, ultimately resulting in cell death. AMG 900 exhibits acceptable PK properties in preclinical species and is predicted to have low clearance in humans. Male rats metabolize AMG 900 primarily through hydroxylation with subsequent sulfate conjugation on the pyrimidinyl-pyridine side-chain, whereas female rats favor oxidation on the thiophene ring's methyl group, which is then metabolized to a carboxylic acid, attended by conjugation to an acyl glucuronide. At low-nM concentrations, AMG 900, whether administered alone or in combination with microtubule-targeting drugs (paclitaxel or ixabepilone), may be an effective intervention strategy for the treatment of metastatic breast cancer and provide potential therapeutic options for patients with multidrug-resistant tumors. It is, in fact, also active against taxaneresistant tumor cell lines.

AMG 900 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


AMG 900 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 95)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32820 60
Hubei xin bonus chemical co. LTD
86-13657291602
linda@hubeijusheng.com CHINA 22963 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 31991 58
Career Henan Chemica Co
+86-0371-86658258 +8613203830695
laboratory@coreychem.com China 30241 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 23325 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471
sales@sarms4muscle.com China 10473 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc.

support@targetmol.com United States 38460 58

  • N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine AMG 900
  • AMG 900
  • N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine
  • N-(4-((3-(2-Aminopyrimidin-4-yl)pyridin-2-yl)oxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1
  • AMG-900;AMG900
  • 1-Phthalazinamine, N-[4-[[3-(2-amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-
  • AMG 900 USP/EP/BP
  • 945595-80-2
  • C28H21N7OS
  • C28H21N7O5
  • Inhibitor
  • Inhibitors
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