FRAX 486
Tocris Bioscience, part of Bio-Techne | Catalog # 5190
Potent PAK inhibitor; brain penetrant and orally bioavailable
Key Product Details
Description
Potent PAK inhibitor; brain penetrant and orally bioavailable
Product Description
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.Product Specifications
Molecular Weight
513.39
Formula
C25H23Cl2FN6O
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for FRAX 486
For research use only
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