Y06137|cas:2226534-49-0|西域试剂

Y06137,99.90%

产品编号：Bellancom-111503| CAS NO：2226534-49-0| 分子式：C₂₇H₃₂N₄O₂| 分子量：444.57

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货号	价格	库存与货期
Bellancom-111503	￥2000.00	杭州北京（现货）
Bellancom-111503	￥3500.00	杭州北京（现货）
Bellancom-111503	￥9000.00	杭州北京（现货）
Bellancom-111503	￥15000.00	杭州北京（现货）

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Y06137

产品介绍

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 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%.

体内研究

西域 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%.

体内研究

西域 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%.

性状

Solid

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。