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.

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

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

Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.

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.

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].

PROTAC EGFR degrader 6 is a potent PROTAC EGFR degrader that effectively reduces EGFR Del19 levels in HCC827 cells, exhibiting a DC50 of 45.2 nM. It notably promotes apoptosis and induces G1 phase arrest in HCC827 cells [1].

PROTAC EGFR degrader 4 is a potent molecule designed to target and degrade mutant EGFR, effectively inducing degradation of EGFR del19 and EGFR L858R T790M with DC50 values of 0.51 nM and 126 nM, respectively. It significantly inhibits the growth of HCC827 and H1975 cell lines, demonstrating IC50 values of 0.83 nM and 203.1 nM, respectively. The induced degradation of EGFR by this compound is associated with autophagy [1].

EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R T790M C797S and 0.06 nM for EGFR Del19 T790M C797S. It lacks significant inhibitory effects on EGFR WT. Demonstrating anti-proliferative properties, EGFR-IN-82 also inhibits tumor growth in nude mice, rendering it applicable in non-small cell lung cancer research [1].

EGFR-IN-73 (Compound 3f) effectively inhibits the prevalent EGFR mutation, EGFR Del19, with an IC50 value of 119 nM [1].

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).

PROTAC EGFR Degrader 5 (Compound 10), a potent degrader of EGFR Del19 in HCC827 cells, achieves this with a DC50 of 34.8 nM. This compound effectively induces apoptosis in HCC827 cells and causes cell cycle arrest in the G1 phase [1].

HX103, an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe, exhibits selective inhibition towards various EGFR mutations, including EGFR 19 del, EGFR L858R, EGFR wild type, and EGFR T790M, with respective IC50 values of 1.3, 1.5, 4.0, and 977 nM. It is utilized for quantifying active-EGFR to foresee agent sensitivity in NSCLC (non-small cell lung cancer) patients harboring EGFR-activating mutations [1].

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).

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].

Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.

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

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].

Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19 T790M, L858R T790M, Del19, L85R and Wild type EGFR respectively.

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

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].

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.