BRM/BRG1 ATP Inhibitor-1|cas:2270879-17-7|西域试剂

BRM/BRG1 ATP Inhibitor-1,98.04%

产品编号：Bellancom-119374| CAS NO：2270879-17-7| 分子式：C₁₁H₉F₃N₄O₂S| 分子量：318.27

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货号	价格	库存与货期
Bellancom-119374	￥4500.00	杭州北京（现货）
Bellancom-119374	￥8100.00	杭州北京（现货）
Bellancom-119374	￥13000.00	杭州北京（现货）

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BRM/BRG1 ATP Inhibitor-1

产品介绍

BRM/BRG1 ATP Inhibitor-1 (compound 14) 是一种具有口服活性的变构 brahma 同系物 (BRM)/SMARCA2 (SWI/SNF 相关的染色质亚家族成员 2 的基质相关肌动蛋白依赖调节因子) 和 brahma 相关基因 1 (BRG1)/SMARCA4 三磷酸腺苷酶活性双抑制剂，IC₅₀ 值均低于 0.005 μM。BRM/BRG1 ATP Inhibitor-1 具有抗癌活性。

生物活性

BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC₅₀s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.

体外研究

BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells.
BRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC₅₀ (absolute AC₅₀) value of 0.01 μM and in RERF-LC-AI cells with an AAC₅₀ value of 0.01 μM.

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

Cell Proliferation Assay

Cell Line:	SKMEL5 melanoma cells and SBC-5 small cell carcinoma
Concentration:	0-10 μM
Incubation Time:	5 days
Result:	Inhibited the proliferation of SKMEL5 cells with an AAC₅₀ (absolute AC₅₀) value of 0.004 μM and of SBC-5 cells with the AAC₅₀more than 10 μM.

体内研究
(In Vivo)

BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner.

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

Animal Model:	Female athymic nude mice with RERF-LC-AI tumor xenografts
Dosage:	7.5 mg/kg, 20 mg/kg
Administration:	Oral administration; everyday; 3 weeks
Result:	Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively. Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

体内研究

BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner.

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

Animal Model:	Female athymic nude mice with RERF-LC-AI tumor xenografts
Dosage:	7.5 mg/kg, 20 mg/kg
Administration:	Oral administration; everyday; 3 weeks
Result:	Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively. Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

体内研究

BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner.

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

Animal Model:	Female athymic nude mice with RERF-LC-AI tumor xenografts
Dosage:	7.5 mg/kg, 20 mg/kg
Administration:	Oral administration; everyday; 3 weeks
Result:	Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively. Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (785.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1420 mL	15.7099 mL	31.4199 mL
5 mM	0.6284 mL	3.1420 mL	6.2840 mL
10 mM	0.3142 mL	1.5710 mL	3.1420 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 (6.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.54 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 (6.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.54 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 (6.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.54 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。