egfr(wt)

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.

DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM for EGFRWT and 48 nM for EGFRL858R/T790M, capable of occupying the ATP-binding site and demonstrating significant antitumor efficacy.

EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.

EGFRWT/T790M-IN-2 (Compound 7c) is an inhibitor of EGFR T790M/WT with IC50 values of 0.08 and 0.13 μM, respectively. This compound induces apoptosis by arresting the cell cycle at the G0-G1 phase and demonstrates antitumor activity.

EGFRWT/T790M/L858R-IN-1 (compound 10d) is a potent inhibitor of EGFR, demonstrating IC50 values of 0.097, 0.280, and 0.051 μM for EGFRWT, EGFRT790M, and EGFRL858R, respectively. This compound can be utilized in cancer research.

EGFRWT/T790M-IN-1 (Compound 16h) is a dual inhibitor targeting both EGFRWT and EGFRT790M. It can arrest the cell cycle at the G2/M phase and induce apoptosis. Additionally, EGFRWT/T790M-IN-1 exhibits anticancer activity.

EGFRWT/T790M-IN-3 is an irreversible, covalent inhibitor of EGFRWT and EGFRT790M with IC50 values of 28.1 nM and 24.6 nM, respectively. It also inhibits tubulin polymerization, exhibiting an IC50 of 5.1 μM. EGFRWT/T790M-IN-3 demonstrates significant antiproliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 μM and 4.12 μM, respectively. This compound is applicable in research pertaining to cancers such as non-small cell lung cancer, colon cancer, and breast cancer.

Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.

EGFR-IN-3 is an EGFR inhibitor with potential antitumour activity.EGFR-IN-3 inhibits EGFRwt-TK and induces apoptosis (cell death), which can cause cells to block in the G2/M phase.

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

EGFR-IN-55 is a potent inhibitor of EGFR, acting on EGFRWT (IC50: 70 nM) and EGFRL858R/T790M (IC50: 3.9 nM). EGFR-IN-55 was able to block the cell cycle of NCI-H1975 cells in G0/G1 phase, exhibiting anticancer effects.

Afatinib (BIBW 2992) oxalate is an irreversible, orally active bispecific inhibitor of the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFRwt, 0.4 nM for EGFRL858R, 10 nM for EGFRL858R/T790M, and 14 nM for HER2. Afatinib oxalate can be used to study esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer.

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

EGFR-IN-75, an inhibitor of both EGFR WT and EGFR T790M, exhibits anticancer and antioxidant properties with IC50 values of 0.28 μM and 5.02 μM, respectively.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.

EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.

PF-06459988 is a novel, effective, orally active, irreversible, and selective epidermal growth factor receptor (EGFR) mutant inhibitor. PF-06459988 has high efficiency and high affinity for EGFRs double mutants containing T790M, and has minimal activity against WT EGFR. PF-06459988 makes a candidate drug for the treatment of cancer.

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

MS 154N is a negative control for MS 154. The compound exhibits high binding-affinity for WT and L858R-mutant EGFR (Kdvalues are 3 and 4.3 nM, respectively), but does not significantly induce degradation of EGFR mutants.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.