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1A-116 Sale

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.

1A-116 Chemical Structure

Cas No.:1430208-73-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥498.00
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1mg
¥333.00
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5mg
¥736.00
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10mg
¥1,177.00
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25mg
¥2,232.00
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50mg
¥3,348.00
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100mg
¥4,680.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

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.
[2]. Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840-51.

化学性质

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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溶解性数据

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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
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