XZ739, a Cereblon -dependent PROTAC BCL-XL ( Bcl-2 family member) degrader with a DC 50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis
In Vitro
XZ739 (0.001-10 μM; 48 hours) potently reduces the viability of T-ALL MOLT-4, B-ALL RS4; 11, SCLC NCI-H146 cells, and platelets after 48 h treatment with IC 50 s of 10.1, 41.8, 25.3, and 1217 nM, respectively. XZ739 has >100-fold selectivity for MOLT-4 cells over human platelets. XZ739 (1.2-300 nM; 16 hours) induces BCL-XL degradation in MOLT-4 cells. The BCL-XL degradation induced by XZ739 in MOLT-4 is rapid, starting within 2 h; and 8 h after XZ739 treatment, more than 96% of the BCL-XL is degraded with 100 nM of XZ739. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human platelets and MOLT-4 cells Concentration: 0.001, 0.01, 0.1, 1, and 10 μM Incubation Time: 48 hours Result: IC 50 values were 10.1 nM and 1217 nM for MOLT-4 cells and platelets, respectively. Western Blot AnalysisCell Line: MOLT-4 cells Concentration: 1.2, 3.7, 11, 33, 100, 300 nM Incubation Time: 16 hours Result: Dose-dependently induced BCL-XL degradation.
