Tag: BTK

Avitinib is an Irreversible, Mutant-Selective EGFR Inhibitor

The epidermal growth factor receptor (EGFR) belongs to the ErbB family (also known as the EGFR family) of receptor tyrosine kinases (RTK). EGFR family comprises four distinct receptors: the EGFR (ErbB1, HER1), ErbB-2 (HER2, neu in rodents), ErbB-3 (HER3) and ErbB-4 (HER4). It is worth mentioning that EGFR family...

Tirabrutinib is a Selective BTK Inhibitor

The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma membrane via the pleckstrin homology domain. In humans, BTK mutations result in arrested B-cell development. Besides, it leads to...

Pirtobrutinib is an Orally Active, Highly Selective and non-Covalent BTK Inhibitor

Bruton’s tyrosine kinase (BTK) is a non-receptor kinase that plays a crucial role in oncogenic signaling. It is critical for the proliferation and survival of leukemic cells in many B cell malignancies. BTK has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases...

SJF620 is a Potent PROTAC BTK Degrader

Bruton’s tyrosine kinase (BTK) is an enzyme encoded by the BTK gene in human. BTK is critical for the survival of B-cell neoplasms. BTK plays a crucial role in B cell development, differentiation, and signaling. Inhibition of BTK kinase activity is an important and practical way of treating Non-Hodgkin’s...

XMU-MP-3 is a Potent Non-Covalent BTK Inhibitor and Induces Apoptosis

BTK, a nonreceptor tyrosine kinase member of the Tec kinase family, plays a significant role in B-cell development. BTK is a unique therapeutic target in B-cell malignancies. XMU-MP-3, a noncovalent inhibitor with potent BTK inhibitory. XMU-MP-3 suppresses BTK kinase activity both in vitro and in vivo. In addition, XMU-MP-3...

CNX-500 is a Covalent Btk Inhibitor (CC-292) Linked to Biotin Chemically

Bruton’s tyrosine kinase (Btk) is a kinase. B cells and myeloid cells expressed exclusively. It plays a vital role in B cells. Btk plays an essential role in the B cell receptor (BCR) signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn...