AZD8931
- CAS NO.:848942-61-0
- Empirical Formula: C23H25ClFN5O3
- Molecular Weight: 473.93
- MDL number: MFCD18385011
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:03
What is AZD8931?
The Uses of AZD8931
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.
What are the applications of Application
AZD8931 is a potent inhibitor of EGFR phosphorylation
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.
Properties of AZD8931
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) |
color | White to off-white |
Safety information for AZD8931
Computed Descriptors for AZD8931
New Products
Tubulysin H (R)-tert-butyl (4-methyl-1-oxopentan-3-yl)carbamate (2S,4R)-4-amino-2-methyl-5-phenylpentanoic acid hydrochloride Tubulysin I Diethyl Aluminium Cyanide (1.0 M in Toluene) 2,2-Difluoropropylamine hydrochloride 2,2-Difluoropropanol 1,2,3,6-TETRAHYDROPYRIDINE HYDROCHLORIDE 4,4-DIFLUOROPIPERIDINE 4,4-DIFLUOROCYCLOHEXANAMINE CYCLOBUTYLAMINE HYDROCHLORIDE 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Imeglimin Hydrochloride IH (R)-Methanesulfonic acid 3-(3-fluoro-4- morpholin-4-yl- phenyl)-2-oxo- oxazolidin-5-ylmethyl 3-(S)-(+)- (1-Cyano-1,1- diphenylmethyl)- 1-tosylpyrrolidine Magnesium Trisilicate Latanoprostene Bunod Lubiprostone Flame Retardant Zinc Borate 7-Methoxyquinoline-4-carbonitrileRelated products of tetrahydrofuran
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