Y06137 |
Catalog No.GC33264 |
Y06137 est un inhibiteur puissant et sélectif de BET pour le traitement du cancer de la prostate résistant À la castration (CRPC). Y06137 se lie au bromodomaine BRD4(1) avec un Kd de 81 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2226534-49-0
Sample solution is provided at 25 µL, 10mM.
Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM[1]. Antitumor activity[1].
Y06137 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC50: 0.29-2.6 μμ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06137 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels[1].|| Cell Viability Assay[1]||Cell Line:|LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells |Concentration:|0.001-100 μM|Incubation Time:|96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP|Result:|Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively.|| Western Blot Analysis[1]||Cell Line:|22Rv1 cells|Concentration:|1, 2, 4, 8, and 16 μM|Incubation Time:|48 hours|Result:|Resulted in significant down-regulation of both AR-fl and AR variants levels.
Y06137 (50 mg/kg, i.p. injection, 5 times per week, 25 days) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06137 is well tolerated in the treated mice, based on the weight of the animal body and their general behavior[1].|| Animal Model:|Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) with C4-2B mouse xenograft model[1]|Dosage:|50 mg/kg, 100 μL|Administration:|Intraperitoneal (i.p.) injection, 5 times per week, 25 days|Result:|Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 51%.
[1]. Zhang M, et al. Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC). J Med Chem. 2018 Apr 12;61(7):3037-3058.
Average Rating: 5
(Based on Reviews and 12 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *