Y06137

Research use only, not for human use.

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.(In Vitro):Treatment of AR-positive prostate cancer cell lines 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. Y06137 (0.001-100 nM) exhibits low micromolar or nanomolar potencies in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively.(In Vivo):Y06137 (50 mg/kg, i.p.,100 μL) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06137 exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 51%.

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. Cell Viability Assay Cell 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 IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively.Western Blot Analysis Cell 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.

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. Animal Model:Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid 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%.

——

Chromatin/Epigenetic

Epigenetic Reader Domain

Human Endogenous Metabolite

——

——

2226534-49-0

444.57

C27H32N4O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (140.59 mM)

CC1=NOC(C1=C2)=CC=C2C3=NC(C=C4)=C(N3CC5CCCCC5)C=C4N6CCOC[C@@H]6C

——

(-20℃)

With Ice Pack

≥ 2 years