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Tocris/FRAX 486/5190/10/10 mg

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货号: 5190/10

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

FRAX 486 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 513.39. Batch specific molecular weights may vary from batch to batch due to solvent 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	1.95 mL	9.74 mL	19.48 mL
5 mM	0.39 mL	1.95 mL	3.9 mL
10 mM	0.19 mL	0.97 mL	1.95 mL
50 mM	0.04 mL	0.19 mL	0.39 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Hayashi-Takagi et al (2013) PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc.Natl.Acad.Sci.U.S.A. 111 6461 PMID: 24706880

Dolan et al (2013) Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc.Natl.Acad.Sci.U.S.A. 110 5671 PMID: 23509247

Wang et al (2016) 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 11 e0153312 PMID: 27071060

Keywords: FRAX 486, supplier, FRAX486, potent, p21, activated, kinase, PAK, inhibitors, inhibits, neuroprotective, brain, penetrant, orally, bioavailable, P21-activated, Kinases, P21-activated, Kinases, Tocris Bioscience

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