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Stattic

Stattic是第一个非肽类小分子，有效抑制STAT3激活和核易位，IC50为5.1 μM，高选择性作用于STAT1。

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生物活性

Stattic is reported to selectively inhibit dimerization, activation and nuclear translocation of STAT3. It can also induce the apoptosis of STAT3-dependent breast cancer cell lines.The inhibition of STAT3 by Stattic results in decreased STAT3-mediated HIF-1 expression and subsequent radiosensitization of HNSCC cells. Inhibiting the STAT3 signaling pathway may represent an effective strategy in the treatment of HNSCC. The evidence of Stattic activity in vivo has also been found. Stattic pre-treatment sensitizes orthotopic xenograft HNSCC tumors to radiation, wich results in signiﬁcantly reduced tumor growth, although this effect was not as dramatic as anticipated by the in vitro studies.
体外研究
体内研究
激酶实验
细胞实验

~2.5 μM
动物实验

每天3.75 mg/kg 腹腔注射
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Schust et al (2006) Stattic: a small-molecule inhibitor of STAT3 activation and dimerization. Chem.Biol. 13 1235.

分子式 C8H5NO4S	分子量 211.19	CAS号 19983-44-9	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO 50 mM	Water Insoluble	Ethanol 5 mM

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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