FRAX 486

Name: FRAX 486
Brand: Tocris Bioscience
SKU: 5190

Tocris Bioscience, part of Bio-Techne | Catalog # 5190

Citations (12)

COA / SDS

Potent PAK inhibitor; brain penetrant and orally bioavailable

Key Product Details

Description:	Potent PAK inhibitor; brain penetrant and orally bioavailable
Chemical Name:	6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
Purity:	≥98% (HPLC)
Molecular Weight:	513.39

View Full Technical Details for FRAX 486

Technical Data
Citations

Biological Activity for FRAX 486

FRAX 486 is a potent p21-activated kinase (PAK) inhibitor (IC₅₀ values are 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively). Blocks and reverses the DISC1 knockdown-induced reduction in dendritic spine size in cortical neurons. Attenuates dendritic spine elimination and enhances spine generation in DISC1 knockdown mice. Ameliorates autism-like behavioral symptoms in fragile X mental retardation 1 (Fmr1) knockout mice. Brain penetrant and orally bioavailable.

Compound Libraries for FRAX 486

FRAX 486 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for FRAX 486

M. Wt	513.39
Formula	C₂₅H₂₃Cl₂FN₆O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1232030-35-1
PubChem ID	68060125
InChi Key	DHKFOIHIUYFSOF-UHFFFAOYSA-N
Smiles	FC1=CC(NC3=NC(N(CC)C(C(C5=CC=C(Cl)C=C5Cl)=C4)=O)=C4C=N3)=CC=C1N2CCNCC2

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 FRAX 486

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	10.27	20

Preparing Stock Solutions for FRAX 486

The following data is based on the product molecular weight 513.39.

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
0.2 mM	9.74 mL	48.70 mL	97.39 mL
1 mM	1.95 mL	9.74 mL	19.48 mL
2 mM	0.97 mL	4.87 mL	9.74 mL
10 mM	0.19 mL	0.97 mL	1.95 mL

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References for FRAX 486

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

Dolan Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc.Natl.Acad.Sci.U.S.A. 2013 PMID: 23509247
Wang P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PLoS One 2016 PMID: 27071060
Hayashi-Takagi PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc.Natl.Acad.Sci.U.S.A. 2013 PMID: 24706880