Sapitinib fumarate
Based on 16 publication(s) in Google Scholar
Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
For research use only. We do not sell to patients.
- CAS No.: 1196531-39-1
- Formula: C31H33ClFN5O11
- Molecular Weight:706.07
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) Sapitinib fumarate
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Pharm Anal. 2025 Dec 10.
- EMBO J. 2025 Nov 3. [Abstract]
- J Transl Med. 2021 Jan 23;19(1):43. [Abstract]
- Cell Rep. 2023 May 29;42(6):112570. [Abstract]
- Bioorg Chem. 2024 Jun:147:107412. [Abstract]
- Mol Cancer Res. 2019 Jan;17(1):20-29. [Abstract]
- Molecules. 2023 Mar 2;28(5):2322. [Abstract]
- Mol Med Rep. 2025 Jun;31(6):165. [Abstract]
- Mol Pharmacol. 2019 Dec;96(6):862-870. [Abstract]
- Thorac Cancer. 2025 Jan;16(1):e15488. [Abstract]
- bioRxiv. 2026 Mar 13.
- World J Exp Med. 2025 Jun 20;15(2):100443. [Abstract]
- bioRxiv. 2025 Jun 7:2025.06.04.657911. [Abstract]
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. October 28, 2021.
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All EGFR Isoforms
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Biological Activity
Chemical Information
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CAS No. 1196531-39-1
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Molecular Weight 706.07
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Formula C31H33ClFN5O11
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SMILES
OC(/C=C/C(O)=O)=O.COC(C(OC1CCN(CC1)CC(NC)=O)=C2)=CC3=C2C(NC4=C(C(Cl)=CC=C4)F)=NC=N3.OC(/C=C/C(O)=O)=O
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Synonyms
AZD-8931 fumarate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (16)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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EMBO J
Tyrosine kinase targeting uncovers oncogenic pathway plasticity in Tasmanian devil transmissible cancers. [Abstract]2025 Nov 3. PMID: 41184587 -
J Transl Med
Role of epidermal growth factor receptor inhibitor-induced interferon pathway signaling in the head and neck squamous cell carcinoma therapeutic response. [Abstract]2021 Jan 23;19(1):43. PMID: 33485341 -
Cell Rep
Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]2023 May 29;42(6):112570. PMID: 37252843 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Mol Cancer Res
Endothelial Cells Promote Colorectal Cancer Cell Survival by Activating the HER3-AKT Pathway in a Paracrine Fashion. [Abstract]2019 Jan;17(1):20-29. PMID: 30131447
Sapitinib fumarate purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):20-29. [Abstract]
Western blotting showed that AZD8931 blocks LPEC-1 CM-induced HER3 and AKT phosphorylation. β-actin is used as the loading control.
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Molecules
Development of an LC-MS/MS Method for Quantification of Sapitinib in Human Liver Microsomes: In Silico and In Vitro Metabolic Stability Evaluation. [Abstract]2023 Mar 2;28(5):2322. PMID: 36903565 -
Mol Med Rep
Identification of the clinical value and biological effects of TTN mutation in liver cancer. [Abstract]2025 Jun;31(6):165. PMID: 40242970 -
Mol Pharmacol
Functional RNAi Screens Define Distinct Protein Kinase Vulnerabilities in EGFR-Dependent HNSCC Cell Lines. [Abstract]2019 Dec;96(6):862-870. PMID: 31554698 -
Thorac Cancer
Establishing a new human lung squamous cell carcinoma cell line, OMUL-1, expressing insulin-like growth factor 1 receptor and programmed cell death ligand 1. [Abstract]2025 Jan;16(1):e15488. PMID: 39552203 -
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World J Exp Med
2025 Jun 20;15(2):100443. PMID: 40546672 -
bioRxiv
Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]2025 Jun 7:2025.06.04.657911. PMID: 40502048 -
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Purity & Documentation
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 Feb 15;16(4):1159-69. [Content Brief]
[2]. Mu Z, et al. 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. J Exp Clin Cancer Res. 2014 May 30;33:47. [Content Brief]
[3]. Barlaam B, et al. Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors. ACS Med Chem Lett. 2013 May 31;4(8):742-6. [Content Brief]
[4]. Wang R, et al. Endothelial Cells Promote Colorectal Cancer Cell Survival by Activating the HER3-AKT Pathway in a Paracrine Fashion. Mol Cancer Res. 2018 Aug 21. pii: molcanres.0341.2018. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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