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Irosustat

产品编号 T4464 CAS 288628-05-7

别名: 667-Coumate, BN83495, STX64

Irosustat (667-Coumate) 是类固醇硫酸酯酶抑制剂(IC50:8 nM)，具有抗乳腺癌作用。

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Irosustat, CAS 288628-05-7

规格	价格/CNY	货期
1 mg	￥ 347	现货
2 mg	￥ 490	现货
5 mg	￥ 828	现货
10 mg	￥ 1,230	现货
25 mg	￥ 2,480	现货
50 mg	￥ 3,730	现货
100 mg	￥ 5,580	现货
1 mL * 10 mM (in DMSO)	￥ 892	现货

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纯度: 98.76%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Irosustat (667-Coumate) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
靶点活性	Steroid sulfatase:IC50:8 nM, Steroid sulfatase (MCF-7 cells):0.2 nM
体外活性	Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor with an IC50 of 8 nM. Irosustat (667 COUMATE) inhibits steroid sulphatase (STS) activity in MCF-7 cells with an IC50 of 0.2 nM. However, it has no effect on the morphology or proliferation of MCF-7 cells at 10 μM.
体内活性	Irosustat potently inhibits rat liver, with inhibition of >90% when at a 1 mg/kg concentration. Irosustat (2 mg/kg, p.o. for 5 d) blocks the uterine growth stimulated by oestrone sulfate (E1S) in ovariectomized rats. Moreover, Irosustat (2, 10 mg/kg, p.o.) plus E1S dose-dependently decreases the growth of NMU-induced mammary tumors in ovariectomized rats. Irosustat (667 COUMATE; 10 mg/kg, p.o.) exhibits 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver.
细胞实验	MCF-7 cells are cultured in growth medium (minimum essential medium (MEM) containing, phenol red, 10% foetal calf serum (FCS) and essential nutrients). When the cells reach 60% confluency, they are treated with Irosustat (0.001-10 μM) in growth medium. After 72 h of incubation, photographs are taken under normal conditions of light and the number of attached cells in each flask is determined using a Coulter cell counter
动物实验	Irosustat is formulated in propylene glycol.RatsLudwig rats bearing mammary tumors are used in the assay. Tumor development is monitored, and animals are ovariectomized when tumors reach 0.8-1.5 cm in diameter. Tumors are allowed to regress over a 12- to 13-day period to confirm their hormone-dependent status. Regrowth of tumors is stimulated with oestrone sulfate (E1S; 50 μg/day, s.c.). When tumors have regrown, animals continue to receive either E1S alone or E1S plus Irosustat at 10 mg/kg/day or 2 mg/kg/day, p.o., until tumor regression has occurred. Tumor volumes are calculated from two measured diameters.

别名	667-Coumate, BN83495, STX64
分子量	309.34
分子式	C14H15NO5S
CAS No.	288628-05-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (177.8 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2327 mL	16.1634 mL	32.3269 mL	80.8172 mL
	5 mM	0.6465 mL	3.2327 mL	6.4654 mL	16.1634 mL
	10 mM	0.3233 mL	1.6163 mL	3.2327 mL	8.0817 mL
	20 mM	0.1616 mL	0.8082 mL	1.6163 mL	4.0409 mL
	50 mM	0.0647 mL	0.3233 mL	0.6465 mL	1.6163 mL
	100 mM	0.0323 mL	0.1616 mL	0.3233 mL	0.8082 mL

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参考文献

1. Purohit A,etal.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,etal.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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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