Molecular structure of AZD8931, CAS Number: 848942-61-0
AZD8931 (CAS 848942-61-0)
Alternate Names:
Sapitinib
Application:
AZD8931 is a potent inhibitor of EGFR phosphorylation
CAS Number:
848942-61-0
Purity:
≥96%
Molecular Weight:
473.93
Molecular Formula:
C23H25ClFN5O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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Technical Information
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SDS & Certificate of Analysis
AZD8931 is an ATP competitive and reversible inhibitor of EGFR (ErbB-1), Neu (ErbB-2) and ErbB-3 (the IC50 values are 4 nM, 3 nM and 4 nM, respectively). It is also a small molecule type I inhibitor of the receptor tyrosine kinase (RTK) family of proteins. It targets the RTKs that are involved in the pathogenesis of a variety of cancers, including non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and renal cell carcinoma (RCC). The compound inhibits the growth, migration, and invasion of cancer cells, as well as induces apoptosis and cell cycle arrest in cancer cell lines. Additionally, AZD8931 inhibits HER2, VEGFR2, the production of pro-inflammatory cytokines, and is also known to inhibit other RTKs, such as PDGFR, FGFR, and c-Met.
AZD8931 (CAS 848942-61-0) References
- 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. | Hickinson, DM., et al. 2010. Clin Cancer Res. 16: 1159-69. PMID: 20145185
- Therapeutic potential of the dual EGFR/HER2 inhibitor AZD8931 in circumventing endocrine resistance. | Morrison, G., et al. 2014. Breast Cancer Res Treat. 144: 263-72. PMID: 24554387
- AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: preclinical activity in HER2 non-amplified inflammatory breast cancer models. | Mu, Z., et al. 2014. J Exp Clin Cancer Res. 33: 47. PMID: 24886365
- Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors. | Barlaam, B., et al. 2013. ACS Med Chem Lett. 4: 742-6. PMID: 24900741
- Metabolic disposition of AZD8931, an oral equipotent inhibitor of EGFR, HER2 and HER3 signalling, in rat, dog and man. | Ballard, P., et al. 2014. Xenobiotica. 44: 1083-98. PMID: 25007130
- The first radiosynthesis of [(11)C]AZD8931 as a new potential PET agent for imaging of EGFR, HER2 and HER3 signaling. | Wang, M., et al. 2014. Bioorg Med Chem Lett. 24: 4455-4459. PMID: 25149507
- Combining AZD8931, a novel EGFR/HER2/HER3 signalling inhibitor, with AZD5363 limits AKT inhibitor induced feedback and enhances antitumour efficacy in HER2-amplified breast cancer models. | Crafter, C., et al. 2015. Int J Oncol. 47: 446-54. PMID: 26095475
- Use of a genetically engineered mouse model as a preclinical tool for HER2 breast cancer. | Creedon, H., et al. 2016. Dis Model Mech. 9: 131-40. PMID: 26721874
- Combination therapy with KRAS siRNA and EGFR inhibitor AZD8931 suppresses lung cancer cell growth in vitro. | Zarredar, H., et al. 2019. J Cell Physiol. 234: 1560-1566. PMID: 30132854
- Synergistic Effect of Novel EGFR Inhibitor AZD8931 and p38α siRNA in Lung Adenocarcinoma Cancer Cells. | Zarredar, H., et al. 2019. Anticancer Agents Med Chem. 19: 638-644. PMID: 30827261
- Functional RNAi Screens Define Distinct Protein Kinase Vulnerabilities in EGFR-Dependent HNSCC Cell Lines. | Hinz, TK., et al. 2019. Mol Pharmacol. 96: 862-870. PMID: 31554698
- Dual Erb B Inhibition in Oesophago-gastric Cancer (DEBIOC): A phase I dose escalating safety study and randomised dose expansion of AZD8931 in combination with oxaliplatin and capecitabine chemotherapy in patients with oesophagogastric adenocarcinoma. | Thomas, A., et al. 2020. Eur J Cancer. 124: 131-141. PMID: 31765988
- Exploring the radiosensitizing potential of AZD8931: a pilot study on the human LoVo colorectal cancer cell line. | Antognelli, C., et al. 2020. Int J Radiat Biol. 96: 1504-1512. PMID: 32910714
- Role of epidermal growth factor receptor inhibitor-induced interferon pathway signaling in the head and neck squamous cell carcinoma therapeutic response. | Korpela, SP., et al. 2021. J Transl Med. 19: 43. PMID: 33485341
- Dual targeting of FGFR3 and ERBB3 enhances the efficacy of FGFR inhibitors in FGFR3 fusion-driven bladder cancer. | Weickhardt, AJ., et al. 2022. BMC Cancer. 22: 478. PMID: 35501832
Inhibitor of:
EB2, EGFR, ErbB-3, ErbB-4, Neu, Olfr541, and Tyrosine Kinase.Activator of:
Ron.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AZD8931, 5 mg | sc-364426 | 5 mg | $260.00 | |||
AZD8931, 10 mg | sc-364426A | 10 mg | $490.00 |