EGFR Inhibitor

EGFR-IN-168 (Compound 9a) is a potent EGFR inhibitor with an IC₅₀ of 0.069 μM. EGFR-IN-168 has antitumor activity.

EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research.

EGFR-IN-215 (Compound 019) is an EGFR inhibitor with IC₅₀ values for the L858R BaF3 and L858R/C797S mutant forms of both ≤ 0.25 μM. EGFR-IN-215 can be used in cancer research.

The Anti-ERBB1/EGFR/HER1 Antibody is a CHO-expressed human antibody that targets ERBB1/EGFR/HER1. The Anti-ERBB1/EGFR/HER1 Antibody consists of a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-ERBB1/EGFR/HER1 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 2.74 μM.

EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC₅₀s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.

Becotatug (powder) (JMT-101) is a humanized IgG1 monoclonal antibody targeting epidermal growth factor receptor (EGFR), and serves as the antibody component of the antibody-drug conjugate Becotatug vedotin (HY-171265). Becotatug (powder) specifically binds to the extracellular domain of EGFR, induces receptor internalization and degradation, blocks the EGFR signaling pathway, and mediates antibody-dependent cellular cytotoxicity. When conjugated to monomethyl auristatin E (MMAE) (HY-15162) via a valine-citrulline cleavable linker, Becotatug (powder) enables targeted delivery of cytotoxic drugs to EGFR-positive tumor cells. Becotatug (powder) can be used for research related to non-small cell lung cancer, nasopharyngeal carcinoma, and head and neck squamous cell carcinoma.

Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC₅₀ values of 23 and 29 nM for recombinant BRaf^V600E and EGFR, respectively.

EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR^{19del/T790M/C797S} and EGFR^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-191 is an anti-tumor agent targeting both EGFR and AKT. EGFR-IN-191 exerts its anti-tumor activity by inducing DNA damage, apoptosis, cell cycle arrest, and inhibition of the PI3K/AKT-EGFR signaling pathway in tumor cells. EGFR-IN-191 can be used in the study of tumors such as triple-negative breast cancer.

Erbicin is a single-chain antibody against the human ErbB2 receptor. Erbicin specifically binds to ErbB2-positive cells, inhibits receptor autophosphorylation, and is internalized by target cells. Erbicin can be used in breast cancer-related research.

MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. MTX-241F is able to penetrate the blood-brain barrier and control tumor growth over the long term. MTX-241F exhibits radiosensitizing activity in patient-derived DIPG neurospheres and may be used in the study of diffuse intrinsic pontine glioma (DIPG).

MM-111 is a bispecific antibody fusion protein targeting the ErbB2/ErbB3 oncogenic unit. MM-111 blocks activation of the PI3K pro-survival pathway. MM-111 binds to the ErbB2 receptor, which localizes the bispecific molecule to ErbB2 over-expressing tumor cells and promotes binding of the anti-ErbB3 arm to the ErbB3 receptor. MM-111 binding to ErbB3 results in inhibition of ErbB3 signaling by blocking the binding of the ErbB3 physiological ligand heregulin. MM-111 can be used for the study of ErbB2 over-expressing breast tumors.

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

Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.

AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC₅₀ of 85 nM. AZ14133346 plays an important role in cancer research.

EGFR-IN-218 is an orally effective EGFR inhibitor with IC₅₀ values of 3.85, 0.40, and 140.5 nM against EGFR^WT, EGFR^L858R/T790M, and EGFR^{L858R/T790M/C797S}, respectively. EGFR-IN-218 inhibits EGFR phosphorylation and downstream ERK1/2 signaling, and exhibits in vivo antitumor activity. EGFR-IN-218 can be used for research on EGFR-mutant non-small cell lung cancer, glioblastoma, and brain metastasis.

Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors.

EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR..

EGFR-TK-IN-2 (compound 10b) is EGFR-TK inhibitor with the IC₅₀ of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth.