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FRAX486
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FRAX486图片
CAS NO:1232030-35-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
FRAX486 是一种PAK抑制剂,对 PAK1,PAK2 和 PAK3 的IC50值分别为 14,33 和 39 nM。
生物活性

FRAX486 is ap21-activated kinase(PAK) inhibitor withIC50s of 14, 33 and 39 nM forPAK1,PAK2andPAK3, respectively.

IC50& Target[2]

PAK1

14 nM (IC50)

PAK2

33 nM (IC50)

PAK3

39 nM (IC50)

体外研究
(In Vitro)

In vitro kinase assays using pure enzymes reveal IC50s for FRAX486 between 10-100 nM for PAK1-3, while the IC50of 779 nM for PAK4 is just below the micromolar range. For FRAX486, an EC50value of 500 nM has been reported from cells (5-50 fold higher than IC50). 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[1].

体内研究
(In Vivo)

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[2].

分子量

513.39

性状

Solid

Formula

C25H23Cl2FN6O

CAS 号

1232030-35-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 21.2 mg/mL(41.29 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9478 mL9.7392 mL19.4784 mL
5 mM0.3896 mL1.9478 mL3.8957 mL
10 mM0.1948 mL0.9739 mL1.9478 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。