BMX is a driver of castration resistance in vitro and in vivo.

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BMX is a driver of castration resistance in vitro and in vivo. BMX is a driver of castration resistance in vitro and in vivo. A and B, VCaP cells in charcoal-stripped serum (CSS)-containing medium were treated with BMX-IN-1 (A) or ibrutinib (B) for 5 days and counted (mean ± SE, n = 4). C, VCaP cells in charcoal-stripped serum-containing medium were treated with 5 μmol/L enzalutamide (ENZ), 5 μmol/L ibrutinib (Ibr), or the combination (Combo) for 5 days (mean ± SE; n = 4). D, Representative images of VCaP cells cultured for 2 to 3 weeks in Matrigel-based 3D system with 5 μmol/L enzalutamide, BMX-IN-1, and/or ibrutinib. E, VCaP subcutaneous xenografts were established in ICR-SCID mice. The mice were castrated once the tumors reached 500 mm3 and then administered vehicle (n = 13), ibrutinib (n = 8), or BMX-IN-1 (n = 8; each at 100 mg/kg/d) by i.p. injection. The results are mean ± SE. F and G, Castration-resistant VCaP xenografts were established and then treated for 4 days with vehicle or 100 mg/kg/d BMX-IN-1 or ibrutinib via i.p. injection. F, Representative sections were stained for cleaved caspase-3. G, Biopsies prior to or post 4-day treatment were analyzed for PSA, TMPRSS2, NKX3.1, or AR mRNA expression by qRT-PCR. Sen Chen et al. Cancer Res 2018;78:5203-5215 ©2018 by American Association for Cancer Research