|1-(3,5-二甲基苯基)-3-(2-(三氟甲基)苯基)胍|CsnPharm

CAS No.: 1430208-73-3

1A-116 Catalog No. CSN24205

1A-116 is a specific Rac1 inhibitor.

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实验方案

技术信息

生物活性

描述As a small GTPase, Rac1 switches between active and inactive states at various subcellular locations that include the plasma membrane, nucleus and mitochondria. Once activated, Rac1 interacts with a range of effectors that then mediate various biological functions^[1]. 1A-116 is a specific Rac1 inhibitor^[2]. 1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305^[2]. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC₅₀ value of 4 µM. A-116 also dramatically impaired Rac1 activation at low micromolar range (1 µM)^[3]. Daily treatment of mice with compound 1A-116 at 3mg/kg reduced about 60% the formation of total metastatic lung colonies. A significant antitumor activity is obtained for macronodules (more than 1 mm in diameter) by treatment with 1A-116 in this highly aggressive breast cancer model. The treatment with 1A-116 reduced the total lung weight compare to the control group, leading to a total weight similar to the average pulmonary weight of Balb/c mice^[3].
作用机制Several hydrogen bonds are established between the guanidine nitrogen atoms and residues Asp57 and Ser71. Moreover, pi-stacking interactions are observed between the methylated aromatic ring of the 1A-116 and the aromatic ring of Trp56.
参考文献

[1] Payapilly A, Malliri A. Compartmentalisation of RAC1 signalling. Curr Opin Cell Biol. 2018 Oct;54:50-56. doi: 10.1016/j.ceb.2018.04.009. Epub 2018 Apr 30. PMID: 29723737.
[2] Gonzalez N, Cardama GA, Comin MJ, Segatori VI, Pifano M, Alonso DF, Gomez DE, Menna PL. Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells. Cell Signal. 2017 Jan;30:154-161. doi: 10.1016/j.cellsig.2016.12.002. Epub 2016 Dec 7. PMID: 27939839.
[3] Cardama GA, Comin MJ, Hornos L, Gonzalez N, Defelipe L, Turjanski AG, Alonso DF, Gomez DE, Menna PL. 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. doi: 10.2174/18715206113136660334. PMID: 24066799; PMCID: PMC4104455.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2540 mL
- 16.2702 mL
- 32.5404 mL
- 5 mM
- 0.6508 mL
- 3.2540 mL
- 6.5081 mL
- 10 mM
- 0.3254 mL
- 1.6270 mL
- 3.2540 mL

技术信息

CAS号

1430208-73-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16F3N3

运输

蓝冰

分子量

307.31

别名

溶解度

DMSO	350.0 mg/mL (1138.9 mM)
Water	insoluble

动物实验配方

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1A-116 Catalog No. CSN24205

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