產(chǎn)品目錄

規(guī)格	10 mM * 1 mL in DMSO 5mg 10mg 50mg 100mg
CAS	1232030-35-1
別名	N/A
化學(xué)名	6-(2,4-dichlorophenyl)-8-ethyl-2-((3-fluoro-4-(piperazin-1-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
分子式	C25H23Cl2FN6O
分子量	513.39
溶解度	<2.59 mg/mL in DMSO, <2.62 mg/mL in ETOH, <2.56 mg/mL in H2O
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

IC50: 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively

FRAX486 is a p21-activated kinase (PAK) inhibitor.

PAKs are known as effector proteins for the Rho GTPases Cdc42 and Rac. Both in vitro and in vivo studies have showed PAKs play critical roles for cytoskeletal organization and in various aspects of cell growth and development.

In vitro: Previous study showed in WPMY-1 cells, FRAX486 could dose-dependently induce the degeneration of actin filaments, which was accompanied by proliferation rate attenuation. Moreover, the FRAX486 cytotoxicity in WPMY-1 cells was found to be both time- and concentration-dependent. In addition, the effects of FRAX486 on actin organization, survival, and proliferation were observed at 1-5 μM in WPMY-1 cells, and complete inhibition of PAK1-3 might be expected, whereas PAK4 might be inhibited only partially at these concentrations [1].

In vivo: Animal study found that FRAX486 was able to cross the blood-brain barrier (BBB) and the brain therapeutical FRAX486 concentrations were detected as early as 1 h and remained as long as 24 h, with the maximum concentration (Cmax) at 8 h. Moreover, FRAX486 could reduce hyperactivity and stereotypical movements, both of which were phenotypes characterizing the Fragile X syndrome mouse model [2].

Clinical trial: Up to now, FRAX486 is still in the preclinical development stage.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗(yàn)證碼*