Zipalertinib (TAS6417; CLN-081; TAS-6417) is a novel, potent, orally bioavailable and selective covalent/irreversible EGFR inhibitor with anticancer activity.
Pyrotinib (SHR-1258) is a selective and orally bioavailable, dual kinase inhibitor of EGFR/HER2 [(epidermal growth factor receptor, or HER-1) and the human epidermal growth factor receptor 2 (ErbB2 or HER-2)] with IC50s of 13 and 38 nM, respectively.
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
JBJ-04-125-02 R-isomer, the R-enantiomer of JBJ-04-125-02, is a novel, highly potent, mutant-specific, allosteric and orally bioavailable EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M.
AV-412 Tosylate (also known as AV412; MP-412), the tosyulate salt of AV412, is a novel, 2nd generation and orally bioavailable EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
Naquotinib mesylate (ASP-8273; ASP8273), the mesylate salt of Naquotinib, is an irreversible/covalent and third-generation epidermal growth factor receptor (EGFR) inhibitor with potential anticancer activity.
NSC228155 is a novel and potent activator of EGFR, which binds to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation.
Nazartinib S-enantiomer is the S-isomer of Nazartinib which is a novel, covalent/irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
Nazartinib mesylate (formerly known as EGF816 mesylate and NVS-816 mesylate) is a novel, covalent/irreversible, and mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
Avitinib maleate (formerly also known as AC-0010, AC0010MA; Abivertinib), the maleate salt of avitinib, is an orally bioavailable and covalent/irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor selective for T790M resistance mutations.