S81347 |
SH5-07 |
源叶(MedMol) | 95% |
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- 产品描述: SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay
- 靶点: STAT3:3.9 μM (IC50);STAT
- 体外研究:
SH5-07 is a hydroxamic acid analog of BP-1-102. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in in vitro assay. It preferentially inhibits Stat3:Stat3 DNA-binding activity, ahead of inhibiting Stat1:Stat3 activity, with minimal effects on Stat1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3 association with growth factor receptor, and thereby inhibits Stat3 phosphorylation. It induces antitumor cell effects against malignant cells harboring constitutively-active Stat3. SH5-07 inhibits the expression of known Stat3-regulated genes. Bcl-2, Bcl-xL, c-Myc, Survivin, Cyclin D1 and Mcl-1 expression is reduced in response to 24 h, 5 μM SH5-07 treatment。
- 体内研究:
Tail vein injection or oral gavage delivery of SH5-07 or SH4-54 inhibits growth of 90-150 mm3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, associated with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity are observed。
- 参考文献:
1. Yue P,et al. Hydroxamic Acid and Benzoic Acid-Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo. Cancer Res. 2016 Feb 1;76(3):652-63.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.598 ml 7.992 ml 15.984 ml 5 mM 0.32 ml 1.598 ml 3.197 ml 10 mM 0.16 ml 0.799 ml 1.598 ml 50 mM 0.032 ml 0.16 ml 0.32 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)