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1A-116 is a specific Rac1 inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $46 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $189 | In Stock | |
25 mg | $378 | In Stock | |
50 mg | $568 | In Stock | |
100 mg | $815 | In Stock | |
500 mg | $1,680 | In Stock | |
1 mL x 10 mM (in DMSO) | $125 | In Stock |
Description | 1A-116 is a specific inhibitor of Rac1 . |
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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (325.40 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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