FRAX597

For research use only. Not for use in humans.

目录号:S7271

FRAX597 Chemical Structure

CAS No. 1286739-19-2

FRAX597是一种有效的,ATP竞争性的第一类PAKs抑制剂,对PAK1,PAK2,和 PAK3 的 IC50 分别为 8 nM,13 nM,和 19 nM。

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客户使用Selleck生产的FRAX597发表文献16篇:

客户使用该产品的3个实验数据:

  • (e) FRAX597 (1 μM) for 1 h, and seeded onto Matrigel. 2F-2B cells were supplemented with exosomes (30 μg). After 24 h culture, tube formation was analysed and imaged. Scale bar = 50 μm. (representative images from n=3, *p<0.05, **p<0.01 and NS = no significant difference).

    Oncotarget, 2016, 7(15):19709-22. FRAX597 purchased from Selleck.

  • Induction of caspase-3 with FRAX597 (2 µM) is enhanced by co-treatment with KJ-Pyr-9 (12.5 µM), as shown by Immunoblotting. All treatments were performed for 30 h.

    Am J Cancer Res, 2017, 7(8):1724-1737. FRAX597 purchased from Selleck.

  • (A) Cells were cultured on glass coverslips and pretreated with IPA3 (5 μM) or FRAX597 (50 nM) for 30 min and subsequently exposed to 1 mM sevoflurane or isoflurane for 30 min. The redistribution of filamentous actin and globular actin was determined by phalloidin–Alexa568 and DNAse I-Alexa488 staining and immunofluorescence microscopy. Magnification, 400 × (the scale bar represents 50 μm). Similar results were obtained in three independent experiments.

    PLoS One, 2016, 11(9):e0162214. FRAX597 purchased from Selleck.

产品安全说明书

PAK抑制剂选择性比较

生物活性

产品描述 FRAX597是一种有效的,ATP竞争性的第一类PAKs抑制剂,对PAK1,PAK2,和 PAK3 的 IC50 分别为 8 nM,13 nM,和 19 nM。
靶点
PAK1 [1]
(Cell-free assay)
PAK2 [1]
(Cell-free assay)
PAK2 [1]
(Cell-free assay)
PAK3 [1]
(Cell-free assay)
8 nM 13 nM 13 nM 19 nM
体外研究

FRAX597 (100 n M)对YES1 (87%),RET (82%),CSF1R (91%),TEK (87%),PAK1 (82%),和PAK2 (93%)表现出显著的抑制作用,而对第二组PAKs:PAK4 (0%),PAK6 (23%),和PAK7 (8%)表现出最低的抑制活性。FRAX597治疗显著减弱Nf2-null SC4 Schwann细胞(SC4 细胞)的增殖。FRAX597抗野生型PAK1的IC50值为48 nM,而抗V342F和V342Y PAK1突变型的IC 50值分别高于3μM和2 μM。[1] FRAX597处理72小时后,抑制benign (Ben-Men1,3μM)和malignant (KT21-MG1, 0.4 μM)脑膜瘤细胞的增殖和能动性。[2]

Assay
Methods Test Index PMID
Western blot
p-PAK1 / PAK1 ; 

PubMed: 23960073     


Western blot analysis of FRAX597 inhibition of PAK1 autophosphorylation (p-PAK1). SC4 cells were treated in culture for 2 h at the indicated FRAX597 concentrations and then extracted for protein. Actin was used as a loading control.

23960073
Growth inhibition assay
Cell proliferation ; 

PubMed: 26774265     


The effect of the selective group 1-PAK inhibitor FRAX597 on cell proliferation of the indicated human pancreatic cancer cell lines was measured using the thymidine-incorporation method. The values for the untreated cells were taken as 100 %. The data represent mean ± SEM, summarised from three independent experiments. Significance is not shown for clarity.

Migration and invasion ; 

PubMed: 26774265     


The effect of the selective group 1-PAK inhibitor FRAX597 on cell migration/invasion of the indicated human pancreatic cancer cell lines was measured using the thymidine-incorporation method. The values for the untreated cells were taken as 100 %. The data represent mean ± SEM, summarised from three independent experiments. Significance is not shown for clarity.

Cell viability ; 

PubMed: 26774265     


The effect of the selective group 1-PAK inhibitor FRAX597 on cell survival of the indicated human pancreatic cancer cell lines was measured using the thymidine-incorporation method. The values for the untreated cells were taken as 100 %. The data represent mean ± SEM, summarised from three independent experiments. Significance is not shown for clarity.

26774265
体内研究 在负荷Nf2-/-SC4 Schwann细胞的NOD/SCID小鼠体内,FRAX597 (100 mg/kg/day, p.o.)比对照组引起更显著的肿瘤生长抑制。[1]在患有原位脑膜瘤的SCID小鼠体内,FRAX597 (90 mg/kg/day, p.o.)显著抑制肿瘤生长。[2]在KrasG12D小鼠体内,FRAX597 (90 mg/kg/day, p.o.)处理引起肿瘤消退以及Erk 与 Akt活性损失。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

酶IC50值的测定:

IC50值使用10个浓度点,非放射性,功能性试验测定,采用基于荧光的偶联酶形式,根据制造商方案(Z’-LYTE@生化检测)进行。激酶活性使用Z’-LYTE@和Adapta@激酶试验测定。
细胞实验:[1]
- 合并
  • Cell lines: SC4细胞
  • Concentrations: 1 μM
  • Incubation Time: 4天
  • Method: 30,000细胞/孔以一式三份接种于12孔培养皿。含有或不含有FRAX597的细胞生长培养基每天更换。在指定时间点,使各个孔中的细胞胰蛋白酶化,并使用Coulter计数器计数。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 患有正位脑膜瘤的SCID小鼠模型
  • Dosages: 90 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 14 mg/mL warmed (25.08 mM)
Ethanol 1 mg/mL (1.79 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 558.10
化学式

C29H28ClN7OS

CAS号 1286739-19-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

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PAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID