Irosustat (STX64)
(Synonyms: STX64; BN83495; 667-Coumate) 目录号 : GC33105
A steroid sulfatase inhibitor
Cas No.:288628-05-7
Sample solution is provided at 25 µL, 10mM.
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STX-64 is a steroid sulfatase inhibitor (IC50 = 0.008 ?M in placental microsomes).1 It also inhibits carbonic anhydrase II (CAII; IC50 = 0.025 ?M).2 STX-64 inhibits LPS-induced production of nitric oxide (NO) and prostaglandin E2 in RAW 264.7 macrophages (IC50s = 85.76 and 0.081 ?M, respectively).3 It reduces rat liver steroid sulfatase activity when administered at a dose of 1 mg/kg.1 STX-64 (2 mg/kg) inhibits estrone sulfate-induced uterine growth and reduces the growth of N-nitroso-N-methylurea-induced, estrone sulfate-maintained mammary tumors in ovariectomized rats.4
1.Malini, B., Purohit, A., Ganeshapillai, D., et al.Inhibition of steroid sulphatase activity by tricyclic coumarin sulphamatesJ. Steroid Biochem. Mol. Biol.75(4-5)253-258(2000) 2.Ho, Y.T., Purohit, A., Vicker, N., et al.Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamatesBiochem. Biophys. Res. Commun.305(4)909-914(2003) 3.Jang, H.-L., El-Gamal, M.I., Choi, H.-E., et al.Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophagesBioorg. Med. Chem. Lett.24(2)571-575(2014) 4.Purohit, A., Woo, L.W., Potter, B.V., et al.In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATECancer Res.60(13)3394-3396(2000)
Cell experiment: | 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[2]. |
Animal experiment: | Rats[1]Ludwig 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[1]. |
References: [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. | |
| Cas No. | 288628-05-7 | SDF | |
| 别名 | STX64; BN83495; 667-Coumate | ||
| Canonical SMILES | O=C1OC2=CC(OS(=O)(N)=O)=CC=C2C3=C1CCCCC3 | ||
| 分子式 | C14H15NO5S | 分子量 | 309.34 |
| 溶解度 | DMSO : ≥ 150 mg/mL (484.90 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2327 mL | 16.1634 mL | 32.3269 mL |
| 5 mM | 0.6465 mL | 3.2327 mL | 6.4654 mL |
| 10 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet