EGFR Inhibitor

EGFR-IN-108 (Compound 12) is a selective and covalent EGFR inhibitor (pIC₅₀: 9.4).

Myristicin (Standard) is the analytical standard of Myristicin. This product is intended for research and analytical applications. Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc.

Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM.

EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent EGFR inhibitor, with IC₅₀s of 0.097, 0.280, and 0.051?μM for EGFR^WT, EGFR^T790M, and EGFR^L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer.

NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC₅₀ of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model.

PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC₅₀s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors.

EGFR WT/T790M-IN-3 is an irreversible covalent EGFR^WT and EGFR^T790M inhibitor with IC₅₀s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC₅₀ value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC₅₀ values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer.

EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC₅₀s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975.

EGFR-IN-118 (Compound 4a) is an inhibitor for the tyrosine kinase EGFR. EGFR-IN-118 demonstrates anti-cancer property, inhibiting the proliferation of MCF-7 and PC3 with IC₅₀ of 2.53 and 3.25 µg/ml. EGFR-IN-118 exhibits antioxidant efficacy, inhibiting the DPPH free radicals with IC₅₀ of 10.04 µg/ml.

Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC₅₀ of 2-37 nM in NR6wtEGFR cells.

Afatinib-d₄ is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

EGFR-IN-35 is a potent inhibitor of EGFR. EGFR-IN-35 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-35 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 11).

GW583340 is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW583340 exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW583340 is applicable to research related to head and neck cancer, breast cancer, and gastric cancer.

EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC₅₀ of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC₅₀ of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.

ADC Control Human IgG1-JSSW-001 is the isotype control for ADC SYS6010 (HY-185832). SYS6010 is an antibody-drug conjugate (ADC) targeting epidermal growth factor receptor (EGFR), which is formed by conjugating the anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) with the topoisomerase I inhibitor JS-1 (HY-178217) via a cleavable tetrapeptide linker. SYS6010 can be used in the research of advanced solid tumors such as non-small cell lung cancer.

EGFR-IN-211 is a EGFR inhibitor with an IC₅₀ of 0.131 μM. EGFR-IN-211 induces cell cycle arrest and apoptosis, and inhibits DNA synthesis and cell division. EGFR-IN-211 can be used in research related to cancers such as colorectal cancer and melanoma.

EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research.

VEGFR-2/c-Met/EGFR-IN-1 is a VEGFR-2/c-Met/EGFR inhibitor with IC₅₀ values of 0.014 μM, 0.072 μM, and 0.94 μM, respectively. c-Met-IN-27 inhibits neovascularization in the chick chorioallantoic membrane (CAM) assay and exhibits in vivo anti-angiogenic activity. c-Met-IN-27 can be used in angiogenesis-related research.

EGFR-IN-84 (Compound 6g) is an EGFR inhibitor (IC₅₀: 24 nM). EGFR-IN-84 inhibits A549 cell growth (IC₅₀: 1.537 μM). EGFR-IN-84 can be used for research of lung cancer.

TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC₅₀ values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations.