Y06137

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Y06137 是一种有效的选择性 BET 抑制剂，对 BRD4(1) 溴结构域的 Kd 为 81 nM。 Y06137可用于去势抵抗性前列腺癌治疗的研究。

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%.

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Chromatin/Epigenetic

Epigenetic Reader Domain

Human Endogenous Metabolite

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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

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(-20℃)

With Ice Pack

≥ 2 years