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Submit ReviewFRAX 486
说明： Potent PAK inhibitor; brain penetrant and orally bioavailable
化学名： 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for FRAX 486
FRAX 486 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for FRAX 486
| 分子量 | 513.39 |
| 公式 | C25H23Cl2FN6O |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for FRAX 486
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 10.27 | 20 |
制备储备液 for FRAX 486
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for FRAX 486
参考文献 for FRAX 486
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 FRAX 486 的引用文献
引用文献是使用了 Tocris 产品的出版物。 FRAX 486 的部分引用包括：
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
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