Tag: ERK

ML786 is an Orally Bioavailable Raf Inhibitor

The mitogen-activated protein kinase (MAPK) signal pathway plays an important role in cells. It also has a response to many different external stimuli and regulates cellular growth, proliferation. The Raf isoform B-Raf is one component of this pathway. Besides, it has a high rate of activating mutation in melanoma...

CPL304110 is an Orally Active and Selective FGFR(1-3) Inhibitor

Over the last decade, the FGFRs family has become an attractive validated therapeutic target notably in cancer. It consists of four members (FGFR1 to FGFR4) which are structurally related cell surface RTKs. This FGF-FGFR axis participates in key biological processes that play significant roles in cell functions such as...

CYH33 is an Orally Active and Highly Selective PI3Kα Inhibitor

PI3Ks are a class of enzymes involved in cell function, such as cell growth, proliferation, differentiation, movement, survival, and intracellular transport. And these cells are relevant to cancer. Specifically, I3K is a kind of related intracellular signal transduction enzymes, which can phosphorylate the 3-hydroxy group of phosphatidylinositol (PtdIns). In...

Balixafortide is a Selective and Well-Tolerated Peptidic CXCR4 Antagonist

Despite the introduction of new targeted therapies and cytotoxic agents, chemotherapy-pretreated metastatic breast cancer (MBC) remains an essentially incurable disease with only moderate median overall survival (OS). over 20 human tumor types overexpress C-X-C chemokine receptor type 4 (CXCR4). CXCR4 levels correlate with aggressive metastatic phenotypes and negative prognosis...

JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor

Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...