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1A-116

Catalog No. T14004Cas No. 1430208-73-3

1A-116 is a specific Rac1 inhibitor.

1A-116

1A-116

Purity: 98.43%
Catalog No. T14004Cas No. 1430208-73-3
1A-116 is a specific Rac1 inhibitor.
Pack SizePriceAvailabilityQuantity
1 mg$46In Stock
5 mg$113In Stock
10 mg$189In Stock
25 mg$378In Stock
50 mg$568In Stock
100 mg$815In Stock
500 mg$1,680In Stock
1 mL x 10 mM (in DMSO)$125In Stock
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Purity:98.43%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight307.31
FormulaC16H16F3N3
Cas No.1430208-73-3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM3.2540 mL16.2702 mL32.5404 mL162.7022 mL
5 mM0.6508 mL3.2540 mL6.5081 mL32.5404 mL
10 mM0.3254 mL1.6270 mL3.2540 mL16.2702 mL
20 mM0.1627 mL0.8135 mL1.6270 mL8.1351 mL
50 mM0.0651 mL0.3254 mL0.6508 mL3.2540 mL
100 mM0.0325 mL0.1627 mL0.3254 mL1.6270 mL

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