egfrwt

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.

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.

(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 0.4 10 14 1 nM for EGFRwt, EGFR (L858R), EGFR (L858R T790M), HER2, and HER4, respectively.

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.

JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R T790M C797S, EGFRWT and EGFRL858R T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.

EGFR-IN-136 (compound 21v) is a potent inhibitor of EGFR, demonstrating IC50 values of 20.2 nM, 1.2 nM, 2.3 nM, and 12.5 nM for EGFRWT, EGFRLR TM, EGFR19D TM CS, and EGFRLR TM CS, respectively. It exhibits antiproliferative and antitumor activities and holds potential for research in non-small cell lung cancer (NSCLC).

EGFR COX-2-IN-1 is an EGFR COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR COX-2-IN-1 significantly increases the proportion of cells in the G2 M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

Rociletinib (CNX-419) is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.

Afatinib impurity 11 is a byproduct of Afatinib, an irreversible EGFR family inhibitor with IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM for EGFRwt, EGFRL858R, EGFRL858R T790M, and HER2, respectively[1].

Zorifertinib (AZD3759) is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK wild-type, and Exon 19Del enzymes, respectively.

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.

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.

EGFR-IN-60 is an effective, orally active, safe antitumor agent. EGFR-IN-60 significantly inhibits EGFRWT (IC50: 83 nM), EGFRT790M (IC50: 26 nM), EGFRL858R (IC50: 53 nM) and JAK3 (IC50: 69 nM). IN-60 inhibited H1975 cells carrying the EGFRT790M mutation (IC50: 1.32 μM) and A431 cells overexpressing EGFRWT (IC50: 4.96 μM). EGFR-IN-60 increased the Bax Bcl-2 ratio, which induced apoptosis induction and cell death.

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.

SPH5030 is an irreversible, selective inhibitor of HER2. SPH5030 inhibits HER2WT (IC50: 3.51 nM), EGFRWT (IC50: 8.13 nM). SPH5030 can be used in cancer research.

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).

(R)-Afatinib ((R)-BIBW 2992), an isomer of Afatinib, is a potent, orally administered, irreversible inhibitor targeting the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFR wt, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R T790M, and 14 nM for HER2, holding potential for research into esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer [1].

EGFR-IN-70 is a potent EGFR inhibitor with IC 50 values of 23.6 and 307.5 nM for EGFR LR TM CS and EGFR WT , respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR . EGFR-IN-70 can be used for cancer research .

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.

EGFRT790M L858R-IN-2 is a potent, selective inhibitor of EGFRT790M L858R, exhibiting IC50 values of 3.5 nM for EGFRT790M L858R and 1290 nM for EGFR WT. This compound effectively decreases the expression of p-EGFR, P-AKT, P-ERK1 2, and induces apoptosis as well as cell cycle arrest in the G1 phase, demonstrating anti-cancer activity [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].