FRAX1036 | PAK Inhibitor | AmBeed-信号通路专用抑制剂

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FRAX1036 {[allProObj[0].p_purity_real_show]}

货号：A374154

FRAX-1036 is a potent and selective PAK1 inhibitor.

FRAX1036 化学结构
CAS号：1432908-05-8

FRAX1036 3D分子结构
CAS号：1432908-05-8

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FRAX1036 纯度/质量文件产品仅供科研

货号：A374154 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

PAK 亚型比较

产品名称	PAK ↓ ↑	PAK1 ↓ ↑	PAK2 ↓ ↑	PAK3 ↓ ↑	PAK4 ↓ ↑	PAK5 ↓ ↑	PAK6 ↓ ↑	纯度
IPA-3	+ PAK1, IC50: 2.5 μM	+ PAK1, IC50: 2.5 μM						{[allProObj[0].p_purity_real_show]}
FRAX486	+++ PAK4, IC50: 39 nM PAK1, IC50: 14 nM	+++ PAK1, IC50: 14 nM	++ PAK2, IC50: 33 nM	++ PAK3, IC50: 39 nM	+ PAK4, IC50: 575 nM			{[allProObj[0].p_purity_real_show]}
FRAX1036	++ PAK2, Ki: 72.4 nM PAK4, Ki: 23.3 nM	++ PAK1, Ki: 23.3 nM	++ PAK2, Ki: 72.4 nM		+ PAK4, Ki: 2.4 μM			{[allProObj[0].p_purity_real_show]}
FRAX597	++++ PAK2, IC50: 13 nM PAK3, IC50: 13 nM	++++ PAK1, IC50: 8 nM	++++ PAK2, IC50: 13 nM	+++ PAK3, IC50: 19 nM				{[allProObj[0].p_purity_real_show]}
PF-3758309	++++ PAK6, Ki: 17.1 nM PAK3, IC50: 190 nM	++++ PAK1, Ki: 13.7 nM	+ PAK2, IC50: 190 nM	++ PAK3, IC50: 99 nM	+++ PAK4, Ki: 18.7 nM	+++ PAK5, Ki: 18.1 nM	+++ PAK6, Ki: 17.1 nM	{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

FRAX1036 生物活性

靶点

PAK

PAK2, Ki:72.4 nM

PAK4, Ki:23.3 nM
PAK1

PAK1, Ki:23.3 nM
PAK2

PAK2, Ki:72.4 nM
PAK4

PAK4, Ki:2.4 μM

描述

The p21-activated kinases (PAKs) have generated significant interest as therapeutic targets in cancer. PAK1 signaling has been shown to be important for regulating cytoskeletal organization and cell migration via both its catalytic activity and protein-protein interactions. FRAX1036, a small molecule pyridopyrimidinone, is a PAK inhibitor. Its biochemical potency (Ki) against PAK1 and PAK2 is 23.3 and 72.4 nM, respectively, with high selectivity against PAK4. Potent cellular inhibition of group I PAK substrate phosphorylation was observed at 2.5 to 5 μM concentrations of FRAX1036 in PAK1-amplified MDA-MB-175 cells. FRAX1036 (5 μM) and docetaxel (0.2 μM) combination treatment for 24 hours of PAK1-amplified lines, MDA-MB-175 and HCC2911, elevated a major apoptotic marker (cleaved PARP) and attenuated a cell cycle regulator (cyclin D1). After 20 hours of treatment with 2.5 μM FRAX1036 for 20 hours, microtubules were disorganized and were not evenly distributed throughout the cytoplasm, between the microtubule organizing center and the periphery. Furthermore, FRAX1036-treated cells completed normal mitoses with the majority of apoptosis occurring during interphase (66.7%)^[3].

FRAX1036 参考文献

[1]Ong CC, Gierke S, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res. 2015 Apr 23;17:59.

[2]Kosoff RE, Aslan JE, et al. Pak2 restrains endomitosis during megakaryopoiesis and alters cytoskeleton organization. Blood. 2015 May 7;125(19):2995-3005.

[3]Ong CC, Gierke S, Pitt C, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res. 2015;17(1):59

FRAX1036 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.65mL

1.93mL

0.97mL

19.30mL

3.86mL

1.93mL

FRAX1036 技术信息

CAS号	1432908-05-8
分子式	C₂₈H₃₂ClN₇O
分子量	518.053

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 4 mg/mL(7.72 mM)，配合水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

FRAX1036 {[allProObj[0].p_purity_real_show]}

FRAX1036 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

FRAX1036 质控信息

FRAX1036 生物活性

FRAX1036 参考文献

FRAX1036 实验方案

FRAX1036 技术信息

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PAK	PAK2, Ki:72.4 nM PAK4, Ki:23.3 nM
PAK1	PAK1, Ki:23.3 nM
PAK2	PAK2, Ki:72.4 nM
PAK4	PAK4, Ki:2.4 μM

FRAX1036 {[allProObj[0].p_purity_real_show]}

FRAX1036 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

FRAX1036 质控信息

FRAX1036 生物活性

FRAX1036 参考文献

FRAX1036 实验方案

FRAX1036 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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B

C

F

G

H

J

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FRAX1036 纯度/质量文件产品仅供科研