keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
APTSTAT3-9R-9R is a STAT3 inhibitor (Ki: 231 nmol/L). STAT3 has been reported to promote the proliferation, survival, metastasis, immune escape, as well as drug resistance of cancer cells, making it a promising target for various diseases. However, though multiple STAT3 inhibitors and its regulatory or effector pathway elements have been identified, bioactive agents are limited.
产品描述 | APTSTAT3-9R-9R is a STAT3 inhibitor (Ki: 231 nmol/L). STAT3 has been reported to promote the proliferation, survival, metastasis, immune escape, as well as drug resistance of cancer cells, making it a promising target for various diseases. However, though multiple STAT3 inhibitors and its regulatory or effector pathway elements have been identified, bioactive agents are limited. |
体外活性 | In vitro: The previous study showed that APTSTAT3-9R bound to STAT3 with high specificity and affinity. Moreover, the addition of a cell-penetrating motif to the peptide to yield APTSTAT3-9R enabled uptake by murine B16F1 melanoma cells. In addition, treatment of various types of cancer cells with APTSTAT3-9R was able to inhibit STAT3 phosphorylation and reduce expression of STAT targets, such as Bcl-xL, cyclin D1, and survivin. As a result, APTSTAT3-9R could suppress the viability and proliferation of cancer cells [1]. |
体内活性 | In vivo: In a previous animal in vivo study, a human lung carcinoma xenograft model was prepared by subcutaneous implantation of A549 cancer cells. After tumors had reached a volume of approximately 50 mm3 after two weeks, APTSTAT3-9R was intratumorally injected every other day for a total of four injections. Results showed that the tumor burden was significantly reduced in the APTSTAT3-9R–treated group when compared with that in the control group; however, there was little difference in tumor size between APTscr-9R and control groups [1]. |
分子量 | 4947.51 |
分子式 | C223H330N80O51 |
CAS No. | TP2222 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Soluble
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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