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Irosustat

Irosustat用途

Irosustat 是一种有效的类固醇硫酸酯酶 (steroid sulfatase) 抑制剂，IC₅₀ 值为 8 nM，具有抗乳腺癌的活性。

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Irosustat名称

[ CAS 号 ]:
288628-05-7

[ 中文名 ]:
Irosustat

[ 英文名 ]:
STX64

[英文别名 ]:

667 Coumate BN 83495
Irosustat
STX64
1ttm
667-Coumate

Irosustat生物活性

[ 描述 ]:

Irosustat 是一种有效的类固醇硫酸酯酶 (steroid sulfatase) 抑制剂,IC50 值为 8 nM,具有抗乳腺癌的活性。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 癌症

[ 靶点 ]

IC50: 8 nM (Steroid sulfatase)[1], 0.2 nM (Steroid sulfatase, MCF-7 cells)[2]

[体外研究]

Irosustat(667 COUMATE)是一种有效的类固醇硫酸酯酶抑制剂,IC50为8 nM [1]。 Irosustat(667 COUMATE)抑制MCF-7细胞中的类固醇硫酸酯酶(STS)活性,IC50为0.2 nM,但对10μM时MCF-7细胞的形态或增殖没有影响[2]。

[体内研究]

Irosustat有效抑制大鼠肝脏,当浓度为1 mg/kg时抑制率> 90％。 Irosustat(2mg/kg,po,持续5天)阻断卵巢切除大鼠中由雌酮硫酸酯(E1S)刺激的子宫生长。此外,Irosustat(2,10 mg/kg,po)加E1S剂量依赖性地减少卵巢切除大鼠中NMU诱导的乳腺肿瘤的生长[1]。 Irosustat(667 COUMATE; 10 mg/kg,po)对大鼠肝脏中的类固醇硫酸酯酶(STS)活性有97.9±0.06％的抑制作用[2]。

[细胞实验]

MCF-7细胞在生长培养基（含有酚红，10％胎牛血清（FCS）和必需营养素的最低必需培养基（MEM））中培养。当细胞达到60％汇合时，在生长培养基中用Iustustat（0.001-10μM）处理它们。孵育72小时后，在正常光照条件下拍摄照片，并使用Coulter细胞计数器[2]测定每个烧瓶中附着细胞的数量。

[动物实验]

大鼠[1]在该测定中使用携带乳腺肿瘤的Ludwig大鼠。监测肿瘤发展，当肿瘤直径达到0.8-1.5cm时，将动物切除卵巢。允许肿瘤在12至13天的时间内消退以确认其激素依赖性状态。用雌酮硫酸盐（E1S;50μg/天，sc）刺激肿瘤的再生长。当肿瘤再生时，动物继续接受单独的E1S或E1S加Iustustat，10mg / kg /天或2mg / kg /天，po，直至肿瘤消退。肿瘤体积由两个测量直径计算[1]。

[参考文献]

[1]. Purohit A, et al. In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATE. Cancer Res. 2000 Jul 1;60(13):3394-6.

[2]. Raobaikady B, et al. Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate. J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):351-8.

[相关活性小分子]

Irosustat物理化学性质

[ 分子式 ]:
C₁₄H₁₅NO₅S

[ 分子量 ]:
309.33800

[ 精确质量 ]:
309.06700

[ PSA ]:
107.98000

[ LogP ]:
3.42530

[ 储存条件 ]:
2-8℃

IrosustatMSDS

详细MSDS(安全技术说明书)

Irosustat安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

Irosustat文献

Evidence of estrone-sulfate uptake modification in young and middle-aged rat prostate.

J. Steroid Biochem. Mol. Biol. 152 , 89-100, (2015)

High plasma exposure to estrogens is often associated with prostate cancer. Reducing this phenomenon may present therapeutic benefits. The involvement of estrone sulphate (E1S), the most abundant circ...

Anti-tumor effect of Shu-Gan-Liang-Xue decoction in breast cancer is related to the inhibition of aromatase and steroid sulfatase expression.

J. Ethnopharmacol. 154(3) , 687-95, (2014)

Shu-Gan-Liang-Xue Decoction (SGLXD), a traditional Chinese herbal formula used to ameliorate the hot flushes in breast cancer patients, was reported to have anti-tumor effect on breast cancer. Estroge...

Inflammatory regulation of steroid sulfatase: A novel mechanism to control estrogen homeostasis and inflammation in chronic liver disease.

J. Hepatol. 64 , 44-52, (2015)

Chronic inflammatory liver diseases are associated with estrogen excess and feminization in men, which is thought to be due to compromised liver function to break down estrogens. The goal of this stud...

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