1A-116

Name: 1A-116
Brand: Tocris Bioscience
SKU: 6701

Tocris Bioscience, part of Bio-Techne | Catalog # 6701

Citations (2)

COA / SDS

Rac1 inhibitor; blocks Rac1-P-Rex1 interaction

Key Product Details

Description:	Rac1 inhibitor; blocks Rac1-P-Rex1 interaction
Chemical Name:	N-(3,5-Dimethylphenyl)-N'-[2-(trifluoromethyl)phenyl]guanidine
Purity:	≥98% (HPLC)
Molecular Weight:	307.31

View Full Technical Details for 1A-116

Technical Data
Citations

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
InChi Key	DVIJFJSZZNOTLP-UHFFFAOYSA-N
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 for 1A-116

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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.

Gonzalez Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells. Cell Signal. 2017 PMID: 27939839
Cabrera Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 2017 PMID: 29228706
Cardama 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 PMID: 24066799