Befotertinib mesylate
Based on 2 publication(s) in Google Scholar
Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 2226167-02-6
- Formula: C30H36F3N7O5S
- Molecular Weight:663.71
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Befotertinib mesylate
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Biological Activity
Befotertinib (0.1-100 μM; 72 h) mesylate exhibits comparable cytotoxic activity in ABCB1-overexpressing KB-V1, NCI-ADR-RES, MDR19-HEK293 cells and their parental cell lines KB-3-1, OVCAR-8, pcDNA3.1-HEK293[1].
Befotertinib (2 μM; 48 h) mesylate enhances Paclitaxel (HY-B0015)-induced apoptosis. After 48 h of combined treatment, the proportion of apoptotic cells increases to 85% in KB-V1 cells and to 95% in NCI-ADR-RES cells[1].
Befotertinib (10 μM; 10 min) mesylate inhibits ABCB1-mediated drug efflux and significantly enhances calcein accumulation in KB-V1, NCI-ADR-RES and MDR19-HEK293 cells after 10 minutes of incubation[1].
Befotertinib (0.001-10000 nM; 72 h) mesylate potently inhibits the proliferation of EGFR-mutant non-small cell lung cancer (NSCLC) cell lines H1975, HCC-827 and H3255, with EC50 values of 1.2 nM, 3.0 nM and 4.3 nM, respectively; whereas it exerts minimal effects on A431 cells overexpressing wild-type (WT) EGFR, with an EC50 value of 1200 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KB-V1, NCI-ADR-RES
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Concentration:2 μM (befotertinib); 1 μM (paclitaxel)
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Incubation Time:48 h
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Result:Induced minimal apoptosis (apoptotic cell populations below 10%) when treated alone in KB-V1 and NCI-ADR-RES cells.
Increased apoptosis to 85% in KB-V1 cells and almost 95% in NCI-ADR-RES cells when co-treated with paclitaxel, comparable to the positive control combination of tariquidar and paclitaxel.
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Cell Line:HCC-827 (delE746-A750), H3255 (L858R), H1975 (L858R/T790M), A431 (WT EGFR overexpressing)
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Concentration:0.001-10000 nM
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Incubation Time:72 h
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Result:Exhibited an antiproliferative EC50 of 1200 nM against A431 WT EGFR-overexpressing cells.
Exhibited an antiproliferative EC50 of 1.2 nM against H1975 L858R/T790M EGFR cells.
Exhibited an antiproliferative EC50 of 3.0 nM against HCC-827 delE746-A750 EGFR cells.
Exhibited an antiproliferative EC50 of 4.3 nM against H3255 L858R EGFR cells.
Chemical Information
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CAS No. 2226167-02-6
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Molecular Weight 663.71
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Formula C30H36F3N7O5S
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SMILES
O=C(NC1=CC(NC2=NC(C3=CN(CC(F)(F)F)C4=C3C=CC=C4)=CC=N2)=C(C=C1N(CCN(C)C)C)OC)C=C.O=S(O)(C)=O
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Synonyms
D-0316 mesylate
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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 (2)
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Journal Impact Factor
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Most Recent
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J Med Chem
2025 Aug 28;68(16):17917-17932. PMID: 40801664 -
Purity & Documentation
References
[1]. Li YC, et al. Befotertinib restored chemosensitivity to multidrug-resistant cancer cells by inhibiting the drug efflux activity of ABCB1. J Pharm Pharmacol. 2026;78(3):rgag020. [Content Brief]
[2]. Damghani T, et al. Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. J Med Chem. 2025;68(16):17917-17932. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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