del19

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains 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 exhibits high kinome selectivity and good DMPK properties.

Almonertinib (HS-10296) is an inhibitor of EGFR activation mutation and tolerant mutation of EGFR T790M, which has only limited activity against wild-type EGFR.

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

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, showcasing its effectiveness by inducing degradation of EGFR del19 and EGFR L858R/T790M with DC50 values of 0.51 nM and 126 nM, respectively. Furthermore, 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, exhibiting an IC50 value of 119 nM [1].

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].

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

EGFR-IN-89 (compound 13k) is a fourth-generation inhibitor selectively targeting EGFR mutations, exhibiting 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-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).

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.

Almonertinib hydrochloride (HS-10296 hydrochloride) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.

Almonertinib mesylate is an irreversible inhibitor of EGFR tyrosine kinase with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate can be used in the non-small cell lung cancer studies.

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).

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