egfrin2

EGFR-IN-2 is a non-covalent, orally available and mutation-selective EGFR inhibitor for the treatment of non-small cell lung cancer (NSCLC), with high selectivity for resistant single and double mutant T790M with IC50 = 27 nm to 33 nM, and low inhibitory activity for wild-type H292 (IC50 = 218 nM).

Mutated EGFR-IN-2 is an inhibitor of mutant-selective EGFR.

SOS1/EGFR-IN-2 (Compound 4) functions as a dual inhibitor of SOS1 and EGFR, exhibiting IC50 values of 8.3 and 14.6 nM, respectively. It demonstrates significant antiproliferative effects on cancer cells harboring various KRAS mutations.

EGFR-IN-26 is an EGFR inhibitor that can be used in cancer research.

EGFR-IN-24 is a potent inhibitor of EGFR and inhibits EGFR (del19/T790M/C797S) and EGFR (L858R/T790M/C797S).

EGFR-IN-25, an efficacious EGFR inhibitor, demonstrates IC50 values of 9 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and 60 nM for A431 cells (WT), respectively.

EGFR-IN-21, a potent EGFR inhibitor, exhibits an IC50 of 0.38 nM, demonstrating significant antitumor activity.

EGFR-IN-23, identified as compound 8 in WO2021244502A1, is a potent EGFR tyrosine kinase inhibitor (TKI) demonstrating an inhibitory concentration (IC50) of 8.05 nM against the BaF3/EGFR-DEL19/T790M/C797S cell line.

EGFR-IN-28 is a potent EGFR inhibitor with demonstrated antitumor activity.

EGFR-IN-29, a potent EGFR inhibitor, demonstrates high efficacy in suppressing epidermal growth factor receptor activity.

EGFR-IN-22 is a highly effective inhibitor targeting wild type EGFR and its mutant form, EGFR L858R/T790M/C797S, displaying IC50 values of 4.91 nM and 0.54 nM, respectively.

ALK/EGFR-IN-2 is a potent dual inhibitor targeting ALK and EGFR, promoting apoptosis and G0/G1 cell cycle arrest in cancer cells. It effectively suppresses proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines, with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively [1].