1A-116
目录号 : GC32770
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes.
Cas No.:1430208-73-3
Sample solution is provided at 25 µL, 10mM.
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes.
[1] Cardama GA, et al. Anticancer Agents Med Chem. 2014;14(6):840-51.
Cell experiment: | 5×103 MCF7::pcDNA.3 and MCF7::C1199 cells are plated in 96-wells plates and 24 hours later are treated for 72 hours with different concentrations of 17-β-Estradiol to evaluate hormone response. To evaluate the reversion of 4-hydroxytamoxifen (Tam) resistance by 1A-116, MCF7::C1199 cells are treated with Tam (0.01 μM, 0.1 μM and 1 μM), 1A-116 (4 μM) or combination of both for 72 hours. Cell growth is measured by colorimetric crystal violet assay. The analysis of hormone-dependent growth and Tam resistance reversion is determined using PRISM 6, Version 6.01. Results shown correspond to the average of three independent experiments[1]. |
Animal experiment: | Specific pathogen-free female BALB/c inbred mice with an age of 8 to 10 weeks and an average weight of 20 g, are used. They are housed in plastic cages under standard conditions and have access to rodent chow and water ad libitum. On day 0, 2×105 viable F3II cells in 0.3 mL Dulbecco’s modified Eagle medium (DMEM) are injected into the lateral tail vein. Mice are injected i.p at daily doses of 3 mg/kg body weight 1A-116 or vehicle. Treatment is carried out from day 0 to day 21. On day 21 mice are sacrificed and lungs are excised and immediately fixed in Bouin’s solution. Superficial lung nodules are counted under dissection microscope[2]. |
References: [1]. Gonzalez N, et al. Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells. Cell Signal. 2017 Jan;30:154-161. |
Cas No. | 1430208-73-3 | SDF | |
Canonical SMILES | N=C(NC1=CC=CC=C1C(F)(F)F)NC2=CC(C)=CC(C)=C2 | ||
分子式 | C16H16F3N3 | 分子量 | 307.31 |
溶解度 | DMSO : 100 mg/mL (325.40 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
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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。 |
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1 mg | 5 mg | 10 mg |
1 mM | 3.254 mL | 16.2702 mL | 32.5404 mL |
5 mM | 0.6508 mL | 3.254 mL | 6.5081 mL |
10 mM | 0.3254 mL | 1.627 mL | 3.254 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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。
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