nci-h1975

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

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.

Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.

EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. It effectively suppresses the proliferation of various lung cancer cells, with IC50 values of 11.7, 5.19, 7.32, and 1.53 μM for NCI-H1781, HCC827, NCI-H3255, and NCI-H1975, respectively. Additionally, EGFR-IN-151 hinders colony formation and cell migration in H1975, induces G1 phase cell cycle arrest, and triggers apoptosis in H1975 cells.

PROTACEGFRdegrader 12 (example 1) is a PROTAC degrader that selectively targets and degrades mutant EGFR, with minimal effect on EGFRWT. It demonstrates an IC50 of less than 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells).

EGFR-IN-165 is a potent EGFR inhibitor with IC50 values of 17.18 nM for EGFRL858R/T790M kinase and 64.74 nM for EGFRWT. Its IC50 values for NCI-H1975 and A431 cell lines are 2.17 μM and 6.2 μM, respectively. EGFR-IN-165 significantly inhibits cell migration, induces G1 phase cell cycle arrest, and causes apoptosis. It is suitable for research on cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

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.

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting agent targeting EGFR L858R/T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI-H1975 cells with an IC50 of 46.82 nM and significantly induces apoptosis and G2/M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R/T790M degrader with a DC50 of 13.2 nM. It effectively inhibits NCI-H1975 cell proliferation with an IC50 of 46.82 nM, induces apoptosis, and causes G2/M phase arrest. This compound shows antitumor activity and is applicable in non-small cell lung cancer (NSCLC) research.

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].

PI3Kα-IN-15 is a powerful inhibitor of PI3Kα, exhibiting an IC₅₀ of 0.15 μM. It shows promising anti-proliferative effects, inhibiting the growth of SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 cell lines with respective IC₅₀ values of 26.6 μM, 7.9 μM, 32.1 μM, 17.7 μM, and 9.4 μM. This compound is useful for cancer research [1].

TAS-121 is an orally active, selective, covalent third-generation mutant EGFR tyrosine kinase inhibitor (EGFR-TKI). It effectively inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM), and Ex19del/T790M mutation (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). TAS-121 also inhibits HER2 and HER4 with an IC50 of 110 nM and 2.6 nM, respectively. This compound prevents cellular proliferation by inhibiting the phosphorylation of EGFR and its downstream signaling targets, thereby inducing apoptosis. Additionally, TAS-121 demonstrates antitumor activity in xenograft models such as SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M).

Cassamine is a diterpene compound isolated from the bark of Erythrophleum fordii. It exhibits cytotoxicity against non-small cell lung cancer cell lines, with IC50 values of 3.4, 2.1, and 1.9 μM for A549, NCI-H1975, and NCI-H1299, respectively. Cassamine possesses antitumor activity and can be applied in research on lung cancer and other tumors.