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1A-116 is a specific Rac1 inhibitor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $46 | In Stock | In Stock | |
| 5 mg | $113 | In Stock | In Stock | |
| 10 mg | $169 | In Stock | In Stock | |
| 25 mg | $297 | In Stock | In Stock | |
| 50 mg | $468 | In Stock | In Stock | |
| 100 mg | $689 | In Stock | In Stock | |
| 200 mg | $973 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $125 | In Stock | In Stock |
| Description | 1A-116 is a specific Rac1 inhibitor. |
| Targets&IC50 | Antiproliferative:4 µM(F3II cell) |
| In vitro | 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[1]. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 μM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 μM)[2]. |
| In vivo | Daily treatment of mice with compound 1A-116 at 3mg/kg body weight/day reduces 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 reduces the total lung weight compare to the control group, leading to a total weight similar to the average pulmonary weight of Balb/c mice[2]. |
| Molecular Weight | 307.31 |
| Formula | C16H16F3N3 |
| Cas No. | 1430208-73-3 |
| Smiles | Cc1cc(C)cc(NC(=N)Nc2ccccc2C(F)(F)F)c1 |
| Relative Density. | 1.22 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (325.40 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (13.02 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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