venetoclax

Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48 245 nM). Venetoclax induces autophagy and apoptosis.

Venetoclax-d8 (ABT-199-d8) is a deuterated form of Venetoclax, a potent, selective, and orally active Bcl-2 inhibitor that induces autophagy and apoptosis.

Venetoclax N-oxide is an impurity of Venetoclax, a highly potent, selective, and orally bioavailable inhibitor of Bcl-2, with a Ki value of less than 0.01 nM (ABT-199; GDC-0199) [1].

Lonitoclax is an inhibitor of B-cell lymphoma 2 (Bcl-2). It demonstrates antitumor activity in B-cell and myeloid malignancy models comparable to Venetoclax. Lonitoclax holds potential for research in relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas.

HDAC3-IN-5 (9c) is a selective inhibitor of HDAC3, exhibiting IC50 values of 4.2 nM for HDAC3, 1629 nM for HDAC2, and 298.2 nM for HDAC1. In vitro, it effectively induces apoptosis in MV4-11 cells and reduces the expression of anti-apoptotic proteins. The development of selective HDAC3 inhibitors like HDAC3-IN-5 (9c) could serve as potential lead compounds for reversing Venetoclax resistance.

ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax.

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

Ara-SH, a derivative of Cytarabine with a mercaptopropionic acid substitution, serves as the initiator for the self-assembly of a smart, co-loaded Cytarabine and Venetoclax nanoparticle (AV-NP), demonstrating notable synergistic antileukemia effects both in vitro and in vivo [1].