|
产品描述： NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM |
|
靶点：
STAT3:86 μM (IC50);STAT |
体内研究：
Human breast (MDA-MB-231) tumor-bearing mice are given an i.v. injection of NSC 74859 (S3I-201) or vehicle every 2 or every 3 days for 2 weeks, and tumor measurements are taken every 2-3 days. Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received S3I-201 display strong growth inhibition. Continued evaluation of treated mice on termination of treatment shows no resumption of tumor growth, suggesting potentially a long-lasting effect of S3I-201 on tumor growth. Compared with vehicle-treated control tumors (n=15), which continued to grow, S3I-201 treatment of somatotroph tumor xenografts (n=15) significantly attenuated tumor growth for the duration of the experiment. Tumors derived from NSC 74859-treated rats are significantly smaller than those from the untreated group (220±16 mm3 vs. 287±16 mm3, P<0.01) as early as 5 days after NSC 74859 injection. Fifteen days after treatments, the average tumor volume of NSC 74859-treated rats is 64% of that of controls (449±40 mm3 vs. 708±83 mm3, P<0.01). Rats are sacrificed and tumors are harvested 15 days after treatment initiation. The average tumor weight of NSC 74859-treated rats is 78±8 mg, while tumors derived from control rats weighed 114±13 mg (32% reduction; P<0.05). |
参考文献：
1. Siddiquee K, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6. 2. Lin L, et al. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-β signaling. Oncogene. 2009 Feb 19;28(7):961-72. 3. Zhou C, et al. STAT3 upregulation in pituitary somatotroph adenomas induces hypersecretion. J Clin Invest. 2015 Apr;125(4):1692-702 |
|
溶解性：
DMSO : 100 mg/mL (273.70 mM; Need ultrasonic) |
|
保存条件：
-20℃ |
配置溶液浓度参考：
|
1mg |
5mg |
10mg |
| 1 mM |
2.737 ml |
13.685 ml |
27.37 ml |
| 5 mM |
0.547 ml |
2.737 ml |
5.474 ml |
| 10 mM |
0.274 ml |
1.369 ml |
2.737 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.547 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京