[CAS NO. 1232030-35-1] FRAX486

Name: FRAX486
Brand: Arctom Scientific
SKU: SLK-S7807

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PRODUCTS SPECIFICATIONS [1232030-35-1]

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Catalog

SLK-S7807

Brand

Selleck

CAS

1232030-35-1

DESCRIPTION [1232030-35-1]

Overview

MDL	-
Molecular Weight	513.39
Molecular Formula	C25H23Cl2FN6O
SMILES	O=C1C(C2=CC=C(Cl)C=C2Cl)=CC3=CN=C(NC4=CC=C(N5CCNCC5)C(F)=C4)N=C3N1CC

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9478 mL	9.7392 mL	19.4784 mL
5 mM	0.3896 mL	1.9478 mL	3.8957 mL
10 mM	0.1948 mL	0.9739 mL	1.9478 mL
50 mM	0.0390 mL	0.1948 mL	0.3896 mL

Description

FRAX486 is a potent inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively.

Targets

PAK1 ^[1] (Cell-free assay)	PAK2 ^[1] (Cell-free assay)	PAK3 ^[1] (Cell-free assay)	PAK4 ^[1] (Cell-free assay)
14 nM	33 nM	39 nM	575 nM

In vitro

In WPMY-1 cells, FRAX486 induces concentration-dependent (1-10 μM) degeneration of actin filaments. This was paralleled by attenuation of proliferation rate, being observed from 1 to 10 μM FRAX486. Cytotoxicity of FRAX486 in WPMY-1 cells is time- and concentration-dependent. In WPMY-1 cells, effects of FRAX486 on actin organization, survival, and proliferation occurred already at concentrations of 1-5 μM. In these concentrations, full inhibition of PAK1-3 may be expected, while PAK4 may be inhibited only partially.

In vivo

FRAX486 crosses the blood-brain barrier and that therapeutically useful concentrations of FRAX486 are in the brain as early as 1 h and remain as long as 24 h after administration, with the maximum concentration in the target tissue at 8 h. Daily dosing results in steady-state levels of FRAX486 in the brain. FRAX486 specifically rescues the Fmr1 KO abnormality in which the spine phenotype is present in apical neurons and not simply decreasing spine density irrespective of genotype or existence of a phenotype. Also, FRAX486 reduces hyperactivity and stereotypical movements, both of which are phenotypes that characterize the mouse model of Fragile X syndrome.

References

[1] Hayashi-Takagi A, et al. Proc Natl Acad Sci U S A. 2014, 111(17):6461-6.
[2] Wang Y, et al. PLoS One. 2016, 11(4):e0153312.
[3] Dolan BM, et al. Proc Natl Acad Sci U S A. 2013, 110(14):5671-6.