Marizomib Salinosporamide A; NPI-0052|cas:437742-34-2|西域试剂

Marizomib Salinosporamide A; NPI-0052,99.55%

产品编号：Bellancom-10985| CAS NO：437742-34-2| 分子式：C₁₅H₂₀ClNO₄| 分子量：313.78

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-10985		￥1500.00	杭州北京（现货）

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Marizomib Salinosporamide A; NPI-0052

产品介绍

Marizomib (Salinosporamide A) 是第二代不可逆的脑渗透性泛蛋白酶体 (proteasome) 抑制剂。Marizomib 抑制 20S 蛋白酶体的 CT-L (β5)、CT-T-laspase 样 (C-L, β1) 和胰蛋白酶样 (T-L, β2) 活性 (IC₅₀ 分别为 3.5, 28, 430 nM)。

生物活性

Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively).

体外研究

Marizomib (Salinosporamide A) (0.1-10000 nM; 72 hours) effectively reduces survival of D-54 and U-251 cells in a dose-dependent manner. The IC₅₀s are ∼52 nM for U-251 and ∼20 nM for D-54.
Marizomib (24 hours; 60 nM) induces apoptosis and caspase-3 activation in glioma cells.

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

Cell Proliferation Assay

Cell Line:	U-251 and D-54 cells
Concentration:	0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:	72 hours
Result:	Effectively reduced survival of D-54 and U-251 cells in a dose-dependent manner.

Apoptosis Analysis

Cell Line:	D-54 cells
Concentration:	60 nM
Incubation Time:	24 hours
Result:	Induces D-54 cells apoptosis.

Western Blot Analysis

Cell Line:	D-54 cells
Concentration:	60 nM
Incubation Time:	24 hours
Result:	Led to increased activity of caspase-3 in a dose-dependent manner.

体内研究
(In Vivo)

Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity.

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

Animal Model:	CB-17 SCID-male mice (4-6 weeks old)
Dosage:	0.15 mg/kg
Administration:	i.v; twice a week for three weeks
Result:	Significantly decreased tumor growth, and was not associated with any toxicity.

体内研究

Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity.

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

Animal Model:	CB-17 SCID-male mice (4-6 weeks old)
Dosage:	0.15 mg/kg
Administration:	i.v; twice a week for three weeks
Result:	Significantly decreased tumor growth, and was not associated with any toxicity.

体内研究

Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity.

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

Animal Model:	CB-17 SCID-male mice (4-6 weeks old)
Dosage:	0.15 mg/kg
Administration:	i.v; twice a week for three weeks
Result:	Significantly decreased tumor growth, and was not associated with any toxicity.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (318.69 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1869 mL	15.9347 mL	31.8695 mL
5 mM	0.6374 mL	3.1869 mL	6.3739 mL
10 mM	0.3187 mL	1.5935 mL	3.1869 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 (6.63 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.63 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 (6.63 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.63 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。