1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes ^{[1] [2]}.

Rac1^[1]

307.31

C₁₆H₁₆F₃N₃

1430208-73-3

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 100 mg/mL (325.40 mM; Need ultrasonic)

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (8.14 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.14 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (8.14 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (8.14 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (8.14 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. 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.

  [2]. Nazareno González, et al. Computational and in vitro Pharmacodynamics Characterization of 1A-116 Rac1 Inhibitor: Relevance of Trp56 in Its Biological Activity. Front Cell Dev Biol. 2020 Apr 15;8:240.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. 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.

  [2]. Nazareno González, et al. Computational and in vitro Pharmacodynamics Characterization of 1A-116 Rac1 Inhibitor: Relevance of Trp56 in Its Biological Activity. Front Cell Dev Biol. 2020 Apr 15;8:240.