FRAX486
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- CAS号:
- 1232030-35-1
- 英文名:
- Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]-
- 英文别名:
- 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
- 中文名:
- FRAX486
- 中文别名:
- FRAX486盐酸盐;FRAX 486,PAK抑制剂;FRAX486是GROUP I PAKS有效抑制剂;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
- CBNumber:
- CB82667850
- 分子式:
- C25H23Cl2FN6O
- 分子量:
- 513.39
- MOL File:
- 1232030-35-1.mol
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FRAX486化学性质
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沸点:
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689.9±65.0 °C(Predicted)
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密度:
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1.403±0.06 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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insoluble in H2O; insoluble in DMSO; insoluble in ETOH
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形态:
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powder
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酸度系数(pKa):
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8.75±0.10(Predicted)
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颜色:
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white to beige
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FRAX486性质、用途与生产工艺
FRAX486 是一种 PAK抑制剂,对 PAK1,PAK2 和 PAK3 的 IC50 值分别为 14,33 和 39 nM。
PAK1
14 nM (IC
50
)
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PAK2
33 nM (IC
50
)
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PAK3
39 nM (IC
50
)
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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.
FRAX486
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-15542B | FRAX486 FRAX486 | 1232030-35-1 | 5mg | 650元 |
2024/08/19 | HY-15542B | FRAX486 FRAX486 | 1232030-35-1 | 10mM * 1mLin DMSO | 730元 |
1232030-35-1, FRAX486 相关搜索:
- 合成有机化合物配体
- 细胞生物学试剂
- 抑制剂
- C25H23Cl2FN6O
- FRAX 486,PAK抑制剂
- 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
- FRAX486盐酸盐
- FRAX486是GROUP I PAKS有效抑制剂
- 1232030-35-1
- FRAX 486; FRAX-486
- 6-(2,4-dichlorophenyl)-8-ethyl-2-((3-fluoro-4-(piperazin-1-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
- CS-1943
- 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-(1-piperazinyl)phen Yl]amino}pyrido[2,3-d]pyrimidin-7(8h)-one FRAX597
- Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]-
- FRAX486