EGFR Inhibitor

EGFR-IN-63 is an EGFR inhibition (IC₅₀: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC₅₀: 2.49 μM).

Adonertinib (FHND9041) is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, which is applicable to research related to advanced non-small cell lung cancer carrying EGFR-sensitive mutations.

AfaPhos1 is a new, Afatinib (HY-10261)-based EGFR PhosTAC. AfaPhos1 induces EGFR dephosphorylation at both pY1068 and pY845. AfaPhos1 induces Apoptosis. AfaPhos1 has anticancer activity against non-small cell lung cancer.

EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC₅₀ of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer.

EGFR-IN-171 is an EGFR inhibitor with an IC₅₀ value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC₅₀ value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer.

Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.

EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC₅₀ values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC₅₀ values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers.

BAT1006 is a monoclonal antibody targeting HER2 extracellular domain II with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) for the study of HER2-positive locally advanced/metastatic solid tumors. BAT1006 has an approximately 5-fold enhanced ADCC effect compared to pertuzumab (HY-P9912) and exhibits potent anti-tumor activity in the HER2-positive Calu-3 xenograft mouse model.

Anti-ERBB3/HER3 (29Z6) is an antibody inhibitor, targeting to human ERBB3/HER3.

EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer.

HTI-1511 Antibody (Halozyme patent anti-EGFR) is a monoclonal antibody inhibitor targeting EGFR. HTI-1511 Antibody can be used to synthesize a novel anti-EGFR-ADC, HTI-1511. HTI-1511 Antibody can be used in the research of head and neck squamous cell carcinoma, non-small cell lung cancer, pancreatic cancer, colorectal cancer, renal cell carcinoma, and epidermoid carcinoma.

EGFR-IN-33 is a potent inhibitor of EGFR. EGFR-IN-33 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-33 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 13).

ERBB3 Human Pre-designed siRNA Set A contains three designed siRNAs for ERBB3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Imgatuzumab (FUT8-KO) is a humanized monoclonal antibody against EGFR expressed in CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Imgatuzumab is an immunomodulator. Imgatuzumab may be used in cancer research.

Delphinidin (chloride) (Standard) is the analytical standard of Delphinidin (chloride). This product is intended for research and analytical applications. Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades.

Panitumumab (ABX-EGF) (powder) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (powder) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (powder) can be used in the research of cancers, such as colon cancer.

HER2-IN-21 (compound 657994) is a human epidermal growth factor receptor 2 (HER2) inhibitor, with an IC₅₀ of 3.85 μM.

EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC₅₀ of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8).

EGFR-IN-112 (SPP10) is an EGFR kinase inhibitor which exhibits IC₅₀s of 2.31 ± 0.3, 3.16 ± 0.8, and 4.2 ± 0.2 μM, against MCF-7, H69AR, and PC-3 cancer cells, respectively. EGFR-IN-112 also demonstrates selective cytotoxicity against cancer cells.