Y06137

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Y06137  纯度: 99.90%

Y06137 是一种有效的选择性 BET 抑制剂，与 BRD4(1) 溴结构域结合，Kd 值为 81 nM。Y06137 用于研究去势抵抗性前列腺癌 (CRPC)。

Y06137

Y06137 Chemical Structure

CAS No. : 2226534-49-0

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10 mM * 1 mL in DMSO ￥2200 In-stock
5 mg ￥2000 In-stock
10 mg ￥3500 In-stock
50 mg ￥9000 In-stock
100 mg ￥15000 In-stock
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500 mg   询价  

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Y06137 相关产品

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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 Kd of 81 nM[1].

IC50 & Target

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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.

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[1].

上海金畔生物科技有限公司 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-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%.

分子量

444.57

Formula

C27H32N4O2
CAS 号

2226534-49-0
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (140.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2494 mL 11.2468 mL 22.4936 mL
5 mM 0.4499 mL 2.2494 mL 4.4987 mL
10 mM 0.2249 mL 1.1247 mL 2.2494 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.68 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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