AZD8931
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- CAS-Nr.
- 848942-61-0
- Englisch Name:
- AZD8931
- Synonyma:
- CS-368;AZD8931;Sapitinib;AZD8931, >=96%;AZD8931 USP/EP/BP;Sapitinib(AZD8931);AZD8931 (Sapitinib);AZD-8931;AZD8931;AZD 8931;AZD8931 (SAPITINIB);AZD 8931;2-[4-({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinaz...
- CBNumber:
- CB22518215
- Summenformel:
- C23H25ClFN5O3
- Molgewicht:
- 473.93
- MOL-Datei:
- 848942-61-0.mol
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AZD8931 Eigenschaften
- Siedepunkt:
- 632.8±55.0 °C(Predicted)
- Dichte
- 1.339
- storage temp.
- Store at -20°C
- L?slichkeit
- ≥23.7 mg/mL in DMSO; insoluble in H2O; ≥57.8 mg/mL in EtOH with gentle warming
- Aggregatzustand
- solid
- pka
- 16.17±0.46(Predicted)
- Farbe
- White to off-white
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
AZD8931 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
AZD8931 is a novel potent reversible small molecule epidermal growth factor receptor, ERBB2 (HER2) and ERBB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively.
Definition
ChEBI: A member of the class of quinazolines that is 4-amino-7-methoxyquinazoline in which the amino group has been substituted by a 3-chloro-2-fluorophenyl group and in which position 6 of the quinoline ring has been substituted by a {1-[2-(methylamino)-2-oxoeth
l]piperidin-4-yl}oxy group. Sapitinib is a dual tyrosine kinase inhibitor (TKI) of epithelial growth factor receptors (EGFR) HER2 and HER3.
Enzyminhibitor
This signal transduction kinase inhibitor (FW = 473.94 g/mol; CAS 848942-61-0), also named 2-(4-[4-(3-chloro-2-fluorophenylamino)-7- methoxyquinazolin-6-yloxy]piperidin-1-yl)-N-methylacetamide, reversibly inhibits EGFR (IC50 = 4 nM), erbB2 (IC50 = 3 nM), and erbB3 (IC50 = 4 nM) phosphorylation in cells. In proliferation assays, AZD8931 is significantly more potent than gefitinib or lapatinib in specific squamous cell carcinoma of the head and neck and non-small cell lung carcinoma cell lines. In vivo, AZD8931 inhibits xenograft growth in a range of models, while significantly affecting EGFR, erbB2, and erbB3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation. In EGF and HRG ligand-driven cell systems, AZD8931 is more potent than gefitinib or lapatinib. Metabolic disposition of AZD8931.
AZD8931 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
AZD8931 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 151)Lieferanten
- 2-[4-[4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide
- AZD8931, >=96%
- AZD8931 (SAPITINIB);AZD 8931
- 4-(3-Chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quina
- AZ08931 2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide
- 2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide
- Sapitinib(AZD8931)
- AZD8931
- 4-(3-Chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline
- Sapitinib
- AZD8931 (Sapitinib)
- CS-368
- AZD-8931;AZD8931;AZD 8931
- 2-[4-({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}oxy)-1-piperidinyl]-N-methylacetamide
- 1-Piperidineacetamide, 4-[[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-methyl-
- AZD8931 USP/EP/BP
- 2-[4-({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinaz...
- 848942-61-0
- C23H25ClFN5O3
- Inhibitors
