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Submit ReviewFRAX 486
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 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 Data for FRAX 486
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 | 48.7 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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Product Datasheets for FRAX 486
References for FRAX 486
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for FRAX 486, please let us know.
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Keywords: FRAX 486, FRAX 486 supplier, FRAX486, potent, p21, activated, kinase, PAK, inhibitors, inhibits, neuroprotective, brain, penetrant, orally, bioavailable, P21-activated, Kinases, 5190, Tocris Bioscience
2 Citations for FRAX 486
Citations are publications that use Tocris products. Selected citations for FRAX 486 include:
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
Teresa L et al (2021) PAK1 Positively Regulates Oligodendrocyte Morphology and Myelination. J Neurosci 41 1864-1877 PMID: 33478987
Do you know of a great paper that uses FRAX 486 from Tocris? Please let us know.
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