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1A-116

Catalog No. T14004   CAS 1430208-73-3

1A-116 is a specific Rac1 inhibitor.

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1A-116 Chemical Structure
1A-116, CAS 1430208-73-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 46.00
5 mg In stock $ 113.00
10 mg In stock $ 189.00
25 mg In stock $ 378.00
50 mg In stock $ 568.00
100 mg In stock $ 815.00
500 mg In stock $ 1,680.00
1 mL * 10 mM (in DMSO) In stock $ 125.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 1A-116 is a specific Rac1 inhibitor.
Targets&IC50 antiproliferation: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

Solubility Information

DMSO: 100 mg/mL (325.40 mM), sonification is recommended.

H2O: < 0.1 mg/mL (insoluble)

TargetMolReferences and Literature

1. Gonzalez N, et al. Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells. Cell Signal. 2017 Jan;30:154-161. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Bioactive Compound Library Inhibitor Library Anti-Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library

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Keywords

1A-116 1430208-73-3 Cell Cycle/Checkpoint Rho TIAM1 inhibit 1A 116 Ras Rho GTPases EGF Apoptosis 1A116 circadian rhythms Inhibitor inhibitor

 

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