Tag: EGFR

Izalontamab (SI-B001) is a Bispecific Anti-EGFR/HER3 mAb for Cancer Research

EGFR (epidermal growth factor receptor) is a member of the ErbB receptor family1. Besides, EGFR is a common therapeutic strategy in epithelioma such as lung adenocarcinoma, colon cancer, head and neck cancer, and esophageal cancer, where the over-expression of EGFR caused by gene mutation plays an essential role in...

Cetuximab (C225) is an Anti-EGFR Monoclonal Antibody for Cancer Research

EGFR (epidermal growth factor receptor) is a transmembrane protein and is a member of the ErbB family. Besides, EGFR is a protein tyrosine kinase expressed on many types of tumor cells, including breast, ovarian, bladder, head and neck, and prostatic carcinoma. Mainly, In malignant tumors, EGFR overexpression is linked...

Amivantamab (JNJ-61186372) is a Human EGFR-MET Bispecific Antibody

Epidermal growth factor (EGF) is a protein that stimulates cell proliferation, differentiation, and survival by binding to its receptor EGFR. Additionally, It exists in platelets, urine, saliva, milk, tears, and blood plasma. The mesenchymal-epithelial transition (MET) is the reverse process of the epithelial-mesenchymal transition (EMT). Moreover, MET involves morphological...

JS25, a Selective and Covalent BTK Inhibitor, Acts by Segregating Tyr551

BTK, Bruton’s tyrosine kinase, belongs to the cytoplasmatic kinases TEC subfamily. BTK involves in immune regulation, and is activated by Src kinases. Then BTK leads to phospholipase-Cγ (PLCγ) phosphorylation, Ca2+ mobilization, and NF-κB/MAP activation. Meanwhile, BTK increases proinflammatory cytokines IL-6 and IL-10 production and controls integrin-mediated B-cells adhesion. Moreover,...

JBJ-09-063 is a Mutant-Selective Allosteric EGFR Inhibitor

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor. And the IC50 values are 0.147 nM, 0.063 nM, 0.083 nM, and 0.396 nM for EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S, and EGFRLT/L747S, respectively. JBJ-09-063 is remarkably effective at inhibiting cell growth. And it also leads to a significant increase in apoptosis. JBJ-09-063 is effective...

EAI001 is a Selective Mutant EGFR Allosteric Inhibitor

Epidermal growth factor receptor (EGFR) belongs to the ErbB family of receptor tyrosine kinases (RTKs). Specifically, EGFR belongs to a receptor family, which contains three additional proteins, namely ErbB-2, ErbB-3, and ErbB-4. These proteins and EGF family growth factors form a comprehensive system. Besides, EGFR participates in cell growth...

BI-1622 is an Orally active and Selective HER2 Inhibitor

BI-1622 is an orally active, potent, and highly selective HER2 (ERBB2) inhibitor, with IC50 values of 7.8, 7.1, <5.3 nM for HER2WT, HER2YVMA, EGFRWT, respectively. Besides, BI-1622 shows greater than 25-fold selectivity over EGFR. Moreover, BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models. HER2 is a member...