|
| | AZD8931 Basic information |
| Product Name: | AZD8931 | | Synonyms: | 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 | | CAS: | 848942-61-0 | | MF: | C23H25ClFN5O3 | | MW: | 473.93 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 848942-61-0.mol |  |
| | AZD8931 Chemical Properties |
| Boiling point | 632.8±55.0 °C(Predicted) | | density | 1.339 | | storage temp. | Store at -20°C | | solubility | ≥23.7 mg/mL in DMSO; insoluble in H2O; ≥57.8 mg/mL in EtOH with gentle warming | | form | solid | | pka | 16.17±0.46(Predicted) |
| | AZD8931 Usage And Synthesis |
| Uses | 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. | | Enzyme inhibitor | 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. | | target | ErbB2 |
| | AZD8931 Preparation Products And Raw materials |
|
