Y06137|2226534-49-0|-陌孚医药/Medlife

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Y06137

目录号: PL13407 纯度: ≥99%

CAS No. :2226534-49-0

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中文名称	Y06137
英文名称	Y06137
英文别名	Y06137;(S)-5-(1-(Cyclohexylmethyl)-6-(3-methylmorpholino)-1H-benzo[d]imidazol-2-yl)-3-methylbenzo[d]isoxazole;5-[1-(Cyclohexylmethyl)-6-[(3S)-3-methylmorpholin-4-yl]benzimidazol-2-yl]-3-methyl-1,2-benzoxazole
Cas No.	2226534-49-0
分子式	C₂₇H₃₂N₄O₂
分子量	444.57
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Y06137 是一种有效的选择性 BET 抑制剂，与 BRD4(1) 溴结构域结合，K_d 值为 81 nM。Y06137 用于研究去势抵抗性前列腺癌 (CRPC)。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	BRD4(1) 81 nM (Kd)
体外研究(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 (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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (140.59 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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