Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a K d of 81 nM In Vitro 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 (IC 50 : 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: AR-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP 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 IC 50 s of 0.47, 0.84, 0.70, 0.29 μM, respectively. Western Blot AnalysisCell Line: AR-positive prostate cancer cell lines 22Rv1 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. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Four-week-old male mice (strain: C.B-17/IcrHsd- Prkdc scid for C4-2B) with C4-2B mouse xenograft model 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%. Form:Solid IC50& Target:BRD4(1) 81 nM (Kd)
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Y06137
CAS number：2226534-49-0 molecular formula：C27H32N4O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2226534-49-0 | molecular formula | C27H32N4O2 |
| molecular weight | 444.57 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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