2226167-02-6
Chemical Structure
Befotertinib mesylate
Synonym(s): D-0316 mesylate
- CAS No.: 2226167-02-6
- Formula:C30H36F3N7O5S
- Molecular Weight:663.71
InChIKey: FFQDXZLQXPZZDJ-UHFFFAOYSA-N
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
Biological Activity: 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[1][2].
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Befotertinib mesylate | 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. | |||||||||||||||||||||
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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]
