Alobresib GS-5829|cas:1637771-14-2|西域试剂

Alobresib GS-5829,98.07%

产品编号：Bellancom-109050| CAS NO：1637771-14-2| 分子式：C₂₆H₂₃N₅O₂| 分子量：437.49

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货号	价格	库存与货期
Bellancom-109050	￥1800.00	杭州北京（现货）
Bellancom-109050	￥3500.00	杭州北京（现货）
Bellancom-109050	￥6800.00	杭州北京（现货）
Bellancom-109050	￥11500.00	杭州北京（现货）
Bellancom-109050	￥0.00	杭州北京（现货）

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Alobresib GS-5829

产品介绍

Alobresib (GS-5829) 是一种 BET 溴结构域抑制剂。Alobresib 可有效对抗复发且耐药的过表达 c-Myc 的子宫浆液性癌。Alobresib 可用于转移性去势抵抗性前列腺癌 (mCRPC) 研究。

生物活性

Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.

体外研究

Alobresib (0.1 nM-100 μM; 72 hours) inhibits cell proliferation in primary uterine serous carcinoma (USC) lines.

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

Cell Proliferation Assay

Cell Line:	Primary uterine serous carcinoma (USC) lines ARK1 and ARK2 cell lines
Concentration:	0.1 nM, 10 nM, 1 μM, 100 μM
Incubation Time:	72 hours
Result:	A progressive, dose response decrease in cell proliferation. IC₅₀s of 27 nM and 31 nM for ARK2 and ARK1 cells, respectively.

体内研究
(In Vivo)

Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) impaires USC-ARK2 xenograft tumor growth in female CB17/lcrHsd-Prkd/scid mice. Alobresib exhibits a significantly slower rate of tumor growth in mice, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).
Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) is well tolerated with no clear impact on body weight compared with vehicle control.

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

Animal Model:	Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors
Dosage:	10 and 20 mg/kg
Administration:	Oral; twice-daily; 28 days
Result:	Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).

体内研究

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

Animal Model:	Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors
Dosage:	10 and 20 mg/kg
Administration:	Oral; twice-daily; 28 days
Result:	Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).

体内研究

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

Animal Model:	Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors
Dosage:	10 and 20 mg/kg
Administration:	Oral; twice-daily; 28 days
Result:	Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (190.47 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2858 mL	11.4288 mL	22.8577 mL
5 mM	0.4572 mL	2.2858 mL	4.5715 mL
10 mM	0.2286 mL	1.1429 mL	2.2858 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 (4.75 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.75 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.75 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.75 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。