Category: Acute Myeloid Leukemia

Talacotuzumab is an IgG1 CD123-Neutralizing Monoclonal Antibody

Interleukin-3 receptor (CD123) is a soluble cytokine that is important for the immune system. CD123 is the receptor of interleukin 3 α Chain is a cytokine receptor. Meanwhile, CD123 is overexpressed in a variety of hematological malignancies. Compared with non-tumor hematopoietic stem cells, CD123 expression was high in leukemia...

Olutasidenib, a Brain-Penetrant Mutant IDH1 Selective Inhibitor For AML Research

On December 1, 2022, FDA approved Rezlidhea (Olutasidenib) to treat adults with relapsed or refractory acute myeloid leukemia (AML) with a susceptible (IDH1) mutation. Olutasidenib (FT2102) is a highly potent, orally active, brain-penetrant, and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1). As a result, The IC50 values are...

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,...

TK4g is a JAK Inhibitor for Leukemia Cancer Research

Janus kinase (JAK) is an intracellular non-receptor tyrosine kinase. There are four members of the JAK family: JAK1, JAK2, JAK3, and Tyrosine kinase 2 (TYK2). JAK can link cytokine signals from membrane receptors to activators of transcription (STAT), transducing cytokine-mediated signals via the JAK-STAT signaling pathway. When the receptor...