Cat. No. Name Size Price Add Cart
KI1303AZD89315 mg$272
AZD893110 mg$512
AZD893150 mg$1552
AZD8931200 mg$3952

Chemical Characteristic

Product NameAZD8931
CAS No.848942-61-0
Molecular Weight 473.93
FormulaC23H25ClFN5O3
Chemical Name2-[4-[4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide
Smilesn1cnc(c2cc(c(cc12)OC)OC1CCN(CC1)CC(=O)NC)Nc1c(c(ccc1)Cl)F
Chemical Structure

Biological activities

AZD8931 is a reversible, ATP competitive inhibitor of epidermal growth factor receptor (EGFR; erbB1), erbB2 (human epidermal growth factor receptor 2), and erbB3 receptor with IC50 of 4, 3 and 4 nM, respectively. In vitro, AZD8931 has greater inhibition of ligand-stimulated EGFR phosphorylation in KB (human buccal carcinoma) cells than gefitinib or lapatinib. In addition, the activity of AZD8931 against the NSCLC cell lines is ranging from insensitivity in NCI-1437 cells with GI50 value of >10 µM to hypersensitivity in PC-9 cells (EGFR activating mutation) with GI50 value of 0.1 nM.[1] In vitro, AZD8931 also has significant and dramatic inhibition effects on the downstream signaling pathways (such as pAKT) , apoptotic, and proliferative endpoints.[2] In BT474c, Calu-3, LoVo, FaDu, and PC-9 xenograft mouse models in vivo, AZD8931 (6.25-50 mg/kg) inhibits xenograft growth while significantly affecting EGFR, erbB2, and erbB3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation.[1]

Protocols

In vivo: AZD8931 is dissolved in polyoxyethylenesorbitan monooleate (Tween 80) in deionized water.[1]

References

[1] Hickinson DM, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res. 2010, 16(4): 1159-1169.
[2] G. Speake, et al. Characterization of AZD8931, a potent reversible small molecule inhibitor against epidermal growth factor receptor (EGFR), erythroblastic leukemia viral oncogene homolog 2 (HER2) and 3 (HER3) with a unique and balanced pharmacological profile. Journal of Clinical Oncology. 2009, 27(15):11072.

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