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)

color 

White to off-white

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(848942-61-0)Related Product Information

• Lapatinib
• MK-2206 2HCl
• Erlotinib hydrochloride
• Ibrutinib
• Afatinib
• Olaparib