Gilteritinib (ASP2215) is a Potent and ATP-competitive FLT3/AXL Inhibitor for AML Research
Acute myeloid leukemia (AML) is a group of malignant diseases of the hematopoietic system. And, AML occurs as the result of mutations in hematopoietic stem/progenitor cells. Despite advances in treatment, AML remains a challenging disease to manage, with a high relapse rate and poor long-term outcomes. In this article,...
TTT 3002 is an Orally Active FLT3 Inhibitor for Acute Myeloid Leukemia Research
TTT-3002, a tyrosine kinase inhibitor is one of the most potent FLT3 inhibitors. FLT3 (Fms-like tyrosine kinase 3, CD135) is a cytokine receptor that belongs to the receptor tyrosine kinase class III. FLT3 is the receptor for the cytokine Flt3 ligand (FLT3L). FLT-3 exists on the surface of many...
Pivekimab sunirine (IMGN 632) is a CD123-targeting ADC for Hematological Malignancies
CD123, the alpha chain of the interleukin 3 receptor (IL-3Rα), is a molecule found on cells that helps transmit the signal for interleukin 3, a soluble cytokine important to the immune system. Besides, Interleukin 3 (IL-3) is a soluble and pleiotropic cytokine. Additionally, IL-3 regulates the function and production...
Navitoclax (ABT-263) is an Orally Active Bcl-2 Inhibitor for Chronic Lymphocytic Leukemia Research
Bcl-2 family proteins, known as B-cell lymphoma 2, are regulators of programmed cell death. Additionally, the bcl-2 family includes pro-apoptotic and anti-apoptotic proteins. Anti-apoptotic proteins refer to Bcl-2, Bcl-x (L), Bcl-w, and Mcl-1. They block apoptosis by isolating pro-apoptotic proteins Bax and Bak. Therefore, one of the main methods...
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...
Rohinitib is a Specific eIF4A Inhibitor Used for Acute Lymphoblastic Leukemia Research
eIF4A is an enzymatic core of the eIF4F complex and an indispensable effector of the mTORC1 pathway. In the first place, eIF4A is a popular target for cancer treatments. Due to the inhibitory effect to translation initiation, eIF4A represses the oncogenic activation of HSF1. Moreover, HSF1 is a factor...
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...