FRAX486
中文名稱 | FRAX486 |
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中文同義詞 | FRAX486是GROUP I PAKS有效抑制劑;FRAX486鹽酸鹽;6-(2,4-二氯苯基)-8-乙基-2-((3-氟-4-(哌嗪-1-基)苯基)氨基)吡啶并[2,3-D]嘧啶-7(8H)-酮;FRAX 486,PAK抑制劑 |
英文名稱 | Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]- |
英文同義詞 | FRAX486;Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]-;6-(2,4-dichlorophenyl)-8-ethyl-2-{[3-fluoro-4-(1-piperazinyl)phen Yl]amino}pyrido[2,3-d]pyrimidin-7(8h)-one FRAX597;6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one;CS-1943;6-(2,4-dichlorophenyl)-8-ethyl-2-((3-fluoro-4-(piperazin-1-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one;FRAX 486; FRAX-486;FRAX486, 10 mM in DMSO |
CAS號 | 1232030-35-1 |
分子式 | C25H23Cl2FN6O |
分子量 | 513.39 |
EINECS號 | |
相關類別 | 抑制劑;細胞生物學試劑 |
Mol文件 | 1232030-35-1.mol |
結構式 | ![]() |
FRAX486 性質
沸點 | 689.9±65.0 °C(Predicted) |
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密度 | 1.403±0.06 g/cm3(Predicted) |
儲存條件 | -20°C |
溶解度 | 不溶于水;不溶于DMSO;不溶于乙醇 |
形態(tài) | 粉末 |
酸度系數(shù)(pKa) | 8.75±0.10(Predicted) |
顏色 | 白色至米色 |
PAK1 14 nM (IC 50 ) |
PAK2 33 nM (IC 50 ) |
PAK3 39 nM (IC 50 ) |
In vitro kinase assays using pure enzymes reveal IC 50 s for FRAX486 between 10-100 nM for PAK1-3, while the IC 50 of 779 nM for PAK4 is just below the micromolar range. For FRAX486, an EC 50 value of 500 nM has been reported from cells (5-50 fold higher than IC 50 ). FRAX486 (30 μM) inhibits endothelin-1 and -2 induced contractions. In WPMY-1 cells, FRAX486 (24 h) induces concentration-dependent (1-10 μM) degeneration of actin filaments. This is 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. FRAX486 significantly reduces the relative proliferation rate in the remaining populations of WPMY-1 cells. While 68% of solvent-treated (24 h) cells shows proliferation, proliferation rate after application of FRAX486 (1-10 μM, 24 h) ranges around 45%. FRAX486 (1-10 μM, 24 h) causes concentration-dependent degeneration of actin filaments. Actin filaments in solvent-treated control cells are arranged to bundles, forming long and thin protrusions, with elongations from adjacent cells overlapping each other. FRAX486 in concentrations of 1 μM causes partial loss of actin organization, including regressing degree of actin polymerization and degeneration of protrusions. FRAX486 in concentrations of 5 or 10 μM causes complete breakdown of filament organization, resulting in a rounded cell shape without protrusions.
FRAX486 displays the highest penetrance of blood–brain barrier in DISC1-knockdown C57BL/6 mice. Daily administration of FRAX486, but not that of vehicle, between P35 and P60 blocks the exacerbated spine loss during adolescence. In addition to the significant blockade of spine elimination, a trend of enhanced spine generation is observed by treatment with FRAX486. FRAX486 treatment ameliorates a deficit in prepulse inhibition in adulthood.
安全信息
更新日期 | 產品編號 | 產品名稱 | CAS號 | 包裝 | 價格 |
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2025/02/08 | HY-15542B | FRAX486 FRAX486 | 1232030-35-1 | 5mg | 650元 |
2025/02/08 | HY-15542B | FRAX486 FRAX486 | 1232030-35-1 | 10mM * 1mLin DMSO | 730元 |