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1232030-35-1

中文名稱 FRAX486
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]-
CAS 1232030-35-1
分子式 C25H23Cl2FN6O
分子量 513.39
MOL 文件 1232030-35-1.mol
更新日期 2024/12/23 17:39:05
1232030-35-1 結(jié)構(gòu)式 1232030-35-1 結(jié)構(gòu)式

基本信息

中文別名
FRAX486是GROUP I PAKS有效抑制劑
英文別名
FRAX486
CS-1943
FRAX 486
FRAX-486
6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
6-(2,4-dichlorophenyl)-8-ethyl-2-((3-fluoro-4-(piperazin-1-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件-20°C
溶解度insoluble in H2O; insoluble in DMSO; insoluble in ETOH
形態(tài)粉末
顏色白色至米色
FRAX486價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-15542BFRAX486
FRAX486
1232030-35-15mg650元
2024/11/08HY-15542BFRAX486
FRAX486
1232030-35-110mM * 1mLin DMSO730元
2024/11/08HY-15542BFRAX486
FRAX486
1232030-35-110mg1100元

常見問題列表

生物活性
FRAX486 是一種 PAK抑制劑,對 PAK1,PAK2 和 PAK3 的 IC50 值分別為 14,33 和 39 nM。
靶點

PAK1

14 nM (IC 50 )

PAK2

33 nM (IC 50 )

PAK3

39 nM (IC 50 )

體外研究

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.

體內(nèi)研究

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.

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