Figure 4. The SET antagonist, OP449, is a potent inhibitor of growth in enzalutamide resistant prostate cancer cells.
(a) Resistant prostate cancer cells show poor response to escalating dosages of enzalutamide in vitro [IC50 (μM): 22RV1 = 35.7, C42 = 37.7, LNCaPENZ−RES = 35.3 and PC3 = 45.73] but are (b,c) highly responsive to OP449 [IC50s (μM): 22RV1 = 5.62, C42 = 2.16, LNCaPENZ−RES, PC3 = 0.67] and (d) in vivo using PC3 cell tumorigenic assays measured by volume or (e) average tumor weight (n=6, treatment starting on day 9, final volume at day 24).