egfr (c797s/del19)

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

ALK-IN-1 is a Brigatinib analog and an ALK inhibitor commonly used in anti-tumor research.

Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.

EGFR-IN-127 is an ATP-competitive inhibitor targeting EGFR, with IC50 values of 136.3 nM for EGFRdel19 and 161.2 nM for EGFRdel19/T790M/C797S. This compound holds potential for the study of non-small cell lung cancer (NSCLC).

DA-0157 is an orally active inhibitor targeting EGFR and ALK, designed to overcome resistance mutations in non-small cell lung cancer (NSCLC). It effectively inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50= 6.9 nM), Ba/F3-EGFR WT (IC50= 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50= 5.5 nM), and Ba/F3-EML4-ALK (IC50= 7.4 nM). Additionally, DA-0157 inhibits CYP2D6 with an IC50 of 5.26 μM and demonstrates antitumor activity in mouse models.

EGFR-IN-98 (Compound 4c) is an EGFR inhibitor, exhibiting IC50 values of 0.277 μM for L858R/T790M/C797S and 0.089 μM for Del19/T790M/C797S enzymes. It is applicable in tumor research.

EGFR-IN-1671 is a selective EGFR inhibitor with an IC50 value of 0.19 nM. It effectively inhibits various EGFR mutants, showing IC50 values of 0.109 nM for EGFR(L858R), 0.75 nM for EGFR(C797S), and less than 0.05 nM for EGFR(del19). EGFR-IN-1671 covalently binds to the catalytically conserved lysine of EGFR in live mammalian cells. By inhibiting EGFR autophosphorylation, this compound demonstrates excellent antiproliferative activity. EGFR-IN-1671 is applicable in research on non-small cell lung cancer (NSCLC), glioblastoma, and various solid tumors.

CH7233163 is a useful organic compound for research related to life sciences and the catalog number is T35334.

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

EGFR-IN-48 is a potent, orally active EGFR inhibitor that acts on EGFRd19/TM/CS (IC50: 0.193 nM), EGFRLR/TM/CS (IC50: 0.251 nM), EGFRWT (IC50: 10.4 nM). EGFR-IN-48 is also able to inhibit EGFR-IN-48 also inhibits the proliferation of BaF3EGFR del19/T790M/C797S cells (IC50: 1.526 nM) and PC-9EGFR del19/T790M/C797S cells (IC50: 66.7 nM).

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-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-69 is a potent inhibitor of the EGFR enzyme, demonstrating IC50 values of 4.3 nM for EGFR L858R/T790M/C797S, 6.6 nM for EGFR L858R/T790M, and 25.6 nM for EGFR 19del/T790M/C797S. This compound is utilized in the research of non-small-cell lung cancer (NSCLC).

EGFR-IN-89 (compound 13k) is a fourth-generation inhibitor that selectively targets EGFR mutations, showing potent activity with an IC50 of 10.1 nM against Del19/T790M/C797S mutations, and demonstrating greater selectivity for mutant forms over wild type [1].

EGFR mutant-IN-2 (Compound D51) is an inhibitor of EGFR mutants, specifically targeting EGFR L858R/T790M/C797S and EGFR del19/T790M/C797S mutants with IC50 values of 14 nM and 62 nM, respectively. This compound exhibits favorable pharmacokinetic (PK) parameters, safety properties, in vivo stability, and demonstrates antitumor activity [1].

EGFR-IN-104 (Compound A23) acts as a potent EGFR inhibitor, demonstrating IC50 values of 0.33 μM for EGFR L858R/T790M and 0.133 μM for EGFR Del19/T790M/C797S. It exhibits anticancer properties, effective both in vitro and in vivo [1].

EGFR-IN-97 (compound 6q), an EGFR inhibitor, demonstrates effectiveness in inhibiting Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, exhibiting IC 50 values of 0.42 μM and 0.41 μM, respectively. Additionally, at a concentration of 0.8 μM, EGFR-IN-97 is capable of inducing apoptosis in NCI-H1975-EGFR L858R/T790M/C797S cells [1].

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.

LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.