Description
AZD8931 can inhibit EGFR and Erbb2 with IC50 of 12 nM and 14 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C23H25ClFN5O3
Chemical Name
2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide
Solubility
DSMO 40 mg/mL Water
In vitro
AZD8931 can inhibit EGFR and Erbb2 with IC50 of 12 nM and 14 nM. AZD8931 has equipotent activity against signaling by three members of this family (epidermal growth factor receptor, erbB2, and erbB3). AZD8931 shows simultaneous, potent inhibition and delivers greater antitumor activity in experimental models than standard agents such as gefitinib or lapatinib. AZD8931 was the most potent inhibitor of erbB2 (IC50, 3 nmol/L) and erbB3 (IC50, 4 nmol/L) phosphorylation and was significantly more potent that either gefitinib or lapatinib for both erbB2.
In vivo
Oral dosing of AZD8931 significantly inhibited BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models.
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