STF-083010
目录号 : KM9128 CAS No. : 307543-71-1 纯度 : ≥98%

STF-083010 是一种 IRE1α 特异性抑制剂。在内质网应激后,STF-083010 抑制 Ire1 内切核酸酶活性,而不影响其激酶活性。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg
In-stock
500mg 询价 In-stock
1g 询价 In-stock

Other Forms of Rapamycin:

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生物活性

STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

体外研究

STF-083010 shows cytostatic and cytotoxic activity in a dose- and time-dependent manner. Treatment with STF-083010 shows significant antimyeloma activity in model human multiple myeloma (MM) xenografts. RPMI 8226 human MM cells grown as tumor xenografts are treated in NSG mice. Intraperitoneal injection of STF-083010 alone (day 1, day 8) significantly inhibits the growth of these tumors. STF-083010 is an IRE1α-specific inhibitor. Four pancreatic cancer cell lines (Panc0403, Panc1005, BxPc3, MiaPaCa2) are treated with different combination of Bortezomib (10 or 50 nM) and STF (10 or 50 μM). The normalized isobologram analysis demonstrates synergistic activity between 10 μM STF and either 10 or 50 nM bortezomib in all four cell lines. Moreover, a higher concentration of STF (50 μM) attains synergy after addition of bortezomib either at a concentration of 10 nM when tested against BxPc3 cells, at a concentration of 50 nM against Panc1005 cells, and at either 10 or 50 nM against Panc0403 cells. STF-083010 (50 μM) suppresses the growth of p53-deficient human cancer cells.

体内研究

Treatment with STF-083010 reduces the viability of HCT116 p53 cells by approximately 20% compared with that of HCT116 p53cells. Administration of STF-083010 to tumors induced by HCT116 p53 cells significantly reduces tumor volume and weight by 75% and 73% at the endpoint, respectively.

分子式
C15H11NO3S2
分子量
317.38
CAS号
307543-71-1
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 : 100 mg/mL (315.08 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1508 mL 15.7540 mL 31.5080 mL
5 mM 0.6302 mL 3.1508 mL 6.3016 mL
10 mM 0.3151 mL 1.5754 mL 3.1508 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: ≥ 3.25 mg/mL (10.24 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (10.24 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 32.5 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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