EGFR Inhibitor

EGFR-IN-214 is an orally active EGFR inhibitor with an EC₅₀ of 3.353 μM. EGFR-IN-214 blocks the downstream PI3K/Akt signaling pathway, induces intracellular ROS accumulation and Caspase-dependent apoptosis. EGFR-IN-214 exhibits antiproliferative activity in cancer cells and inhibits tumor growth in xenograft models. EGFR-IN-214 can be used in studies related to hepatocellular carcinoma.

EGFR-IN-37 is a potent inhibitor of EGFR. EGFR-IN-37 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 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-37 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 7).

EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, which potently targets human EGFR (IC₅₀=0.03 μM), TNF-α (IC₅₀=3.1 μM), and the IL-6/GP130 complex (IC₅₀=1.6 μM). EGFR-IN-200 binds to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, induces G₂/M cell cycle arrest, apoptosis, and antiproliferative activity. EGFR-IN-200 exhibits high gastrointestinal absorbability, low BBB permeability, and complies with the Lipinski's rule. EGFR-IN-200 can be used for the research of lung cancer and breast adenocarcinoma.

anti-NSCLC agent-1 (compound 8dc) is an inhibitor of tyrosine kinase inhibitors (TKIs) with IC₅₀ values of 0.05 and 0.09 μM in A549 and NCI-H441 cells. anti-NSCLC agent-1 shows anti-NSCLC activities in colony formation, migration, and invasion.

EGFR-IN-110 (Compound 6) is a covalent EGFR inhibitor, with pIC₅₀ values of 9.2 and 8.7 for EGFR enzyme and EGFR cell, respectively. EGFR-IN-110 shows high EGFR potency and good kinase selectivity.

EGFR-IN-157 (compound IIB-5) is a potent EGFR inhibitor with an IC₅₀ of 18.81 nM. EGFR-IN-157 can be used in the study of non-small cell lung cancer (NSCLC).

EGFR-IN-38 is a potent inhibitor of EGFR. EGFR-IN-38 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 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-38 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 4).

EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC₅₀s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC₅₀=0.907 μM).

H2Mab-139 (H2Mab-141;H2Mab-19) is an anti-HER2 monoclonal antibody. H2Mab-139 specifically binds to HER2 on various cancer cells. H₂Mab-139 can detect HER2 overexpression in colorectal cancer via flow cytometry and immunohistochemical analysis. H₂Mab-139 exhibits anti-tumor activity in mouse oral cancer and breast cancer xenografts. H2Mab-139 is applicable to research related to multiple cancers including colon cancer, oral cancer, and breast cancer.

EGFR kinase inhibitor 5 (Compound 4c) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC₅₀ of 18.35 μM. EGFR kinase inhibitor 5 induces apoptosis. EGFR kinase inhibitor 5 exhibits anticancer and anti-inflammatory activity with low toxicity (LD₅₀ range: 500-2000 mg/kg).

Lapatinib-d₇ dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFR^T790M kinase inhibitor, with an IC₅₀ of 1.03 nM against FAK and an IC₅₀ of 3.89 nM against EGFR^T790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer.

EGFR-IN-135 (compound 3d) is a EGFR inhibitor with the IC₅₀ of 0.086 μM. EGFR-IN-135 inhibitor cell growth and arrests the cell cycle at the S phase of reast cancer cell lines.

EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC₅₀s of 17.18 and 64.74 nM against EGFR^L858R/T790M and EGFR^WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC₅₀s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively.

EGFR-IN-175 is an orally active and selective EGFR^{L858R/T790M/C797S} inhibitor with an IC₅₀ of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer.

LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR^{19del/T790M/C797S} and EGFR^{L858R/T790M/C797S} with IC₅₀ values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR^{19del/T790M/C797S} and leas to significant tumor regression in a C797S-mutant xenograft model.

VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC₅₀ value of 24.6nM against HCC827 cells.

Asterriquinone (ARQ), a Asterriquinone analog, is a Grb-2 binding inhibitor. Asterriquinone inhibits the Grb-2 binding activity to tyrosine phosphorylated EGFR, with an IC₅₀ of 8.37 μM. Asterriquinone is a HIV1 reverse transcriptase inhibitor with a K_i of 2.3 μM. Asterriquinone also inhibits Grb-7 and PLC-γ binding activities..

EGFR-IN-219 is an EGFR inhibitor. EGFR-IN-219 induces Apoptosis and G0/G1 cell cycle arrest. EGFR-IN-219 exhibits selective anticancer activity against lung adenocarcinoma. EGFR-IN-219 can be used for research on non-small cell lung cancer.