The PROTAC ARCC-4 was synthesized in-house in our laboratories. Based on previously gathered knowledge on the development of AR-targeting PROTACs, we could design a new synthetic route towards a gram-scale synthesis of the desired PROTAC ARCC-4 (for experimental details, see Supplementary Materials ) [32 (link),33 (link),34 (link)]. The obtained material was used in all the subsequent experiments conducted in this study.
HPMCAS (L Grade) was obtained from Shin-Etsu Chemical (Tokyo, Japan), Eudragit® L 100-55 (EL 100-55) from Evonik (Darmstadt, Germany), Copovidone from BASF (Ludwigshafen, Germany), and HPMC HME 15 LV was sent from DuPont Pharma & Nutrition (Luzern, Switzerland). HPC-SSL was kindly donated by Nippon Soda Co., Ltd. (Tokyo, Japan). Silsol 6035 was received from Grace GmbH (Worms, Germany). Propylencarbonat (PC) was purchased from Carl Roth GmbH (Karlsruhe, Germany), and N-Methyl-2-Pyrollidon (NMP) was obtained from VWR International S.A.S. (Rosny-sous-Bois, France). Dimethyl sulfoxide (DMSO, ≥99.9%) was purchased from Fisher Scientific (Geel, Belgium). Di-sodium hydrogen phosphate dihydrate and sodium dihydrogen phosphate dihydrate were obtained from Th. Geyer (Renningen, Germany).
HPMCAS (L Grade) was obtained from Shin-Etsu Chemical (Tokyo, Japan), Eudragit® L 100-55 (EL 100-55) from Evonik (Darmstadt, Germany), Copovidone from BASF (Ludwigshafen, Germany), and HPMC HME 15 LV was sent from DuPont Pharma & Nutrition (Luzern, Switzerland). HPC-SSL was kindly donated by Nippon Soda Co., Ltd. (Tokyo, Japan). Silsol 6035 was received from Grace GmbH (Worms, Germany). Propylencarbonat (PC) was purchased from Carl Roth GmbH (Karlsruhe, Germany), and N-Methyl-2-Pyrollidon (NMP) was obtained from VWR International S.A.S. (Rosny-sous-Bois, France). Dimethyl sulfoxide (DMSO, ≥99.9%) was purchased from Fisher Scientific (Geel, Belgium). Di-sodium hydrogen phosphate dihydrate and sodium dihydrogen phosphate dihydrate were obtained from Th. Geyer (Renningen, Germany).
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