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Description: Rac1 inhibitor; blocks Rac1-P-Rex1 interaction
Chemical Name: N-(3,5-Dimethylphenyl)-N'-[2-(trifluoromethyl)phenyl]guanidine
Purity: ≥98% (HPLC)

Biological Activity for 1A-116

1A-116 is a Rac1 inhibitor. Reduces intracellular Rac1-GTP levels and blocks Rac1-P-Rex1 interaction in vitro. Exhibits no effect on GTPase activity of closely related Cdc42. Displays antiproliferative, anti-invasive and pro-apoptotic activity in several cancer cell lines. Exhibits antimetastatic activity in vivo. Also restores antiproliferative effects of Tamoxifen (Cat. No. 6342) in resistant breast cancer cell.

Licensing Information

Sold under license from Romikin S.A.

Compound Libraries for 1A-116

1A-116 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for 1A-116

M. Wt 307.31
Formula C16H16F3N3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1430208-73-3
PubChem ID 71543346
Smiles CC1=CC(NC(NC2=C(C(F)(F)F)C=CC=C2)=N)=CC(C)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for 1A-116

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 30.73 100
ethanol 30.73 100

Preparing Stock Solutions for 1A-116

The following data is based on the product molecular weight 307.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.25 mL 16.27 mL 32.54 mL
5 mM 0.65 mL 3.25 mL 6.51 mL
10 mM 0.33 mL 1.63 mL 3.25 mL
50 mM 0.07 mL 0.33 mL 0.65 mL

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References for 1A-116

References are publications that support the biological activity of the product.

Cardama et al (2014) Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med.Chem. 14 840 PMID: 24066799

Gonzalez et al (2017) Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells. Cell Signal. 30 154 PMID: 27939839

Cabrera et al (2017) Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 8 98509 PMID: 29228706

If you know of a relevant reference for 1A-116, please let us know.

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Keywords: 1A-116, 1A-116 supplier, rac1, gtpase, inhibitors, inhibits, tamoxifen, resistance, breast, cancer, Rho, 6701, Tocris Bioscience

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