
FRAX1036p21-activated kinase I (PAK1) inhibitor |
Sample solution is provided at 25 µL, 10mM.
































Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure


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Cas No. | 1432908-05-8 | SDF | Download SDF |
Chemical Name | 6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | ||
Canonical SMILES | O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC | ||
Formula | C28H32ClN7O | M.Wt | 518.05 |
Solubility | Soluble in DMSO | Storage | Store at -20°C |
Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
IC50: N/A
FRAX1036 is a p21-activated kinase I (PAK1) inhibitor.
Breast cancer is a clinically and molecularly heterogeneous disease and plenty of genetic and epigenetic studies of breast tumors has revealed novel putative driver genes, such as p21-activated kinase (PAK)1. As a serine/threonine kinase downstream of small GTP-binding proteins including Rac1 and Cdc42, PAK1 is an critical component of growth factor signaling networks and cellular functions important to tumorigenesis.
In vitro: Previous study demonstrated that the administration of docetaxel with either FRAX1036 or PAK1 small interfering RNA oligonucleotides was able to alter signaling to cytoskeletal-associated proteins dramatically, such as stathmin, and also able to induce microtubule disorganization and cellular apoptosis. In addition, the live-cell imaging data showed that the duration of mitotic arrest mediated by docetaxel could be significantly reduced by the treatment of FRAX1036, which was associated with increased kinetics of apoptosis [1].
In vivo: In previous animal study, the untreated mice bearing KT21 transplants showed ventricular invasion, whereas Ben-Men grew at the injection site. Efficacy results found that the treatment with Frax1036 could lead to a slower tumor growth, with reduction in body mass index (BMI) signals of 37% when compared to vehicle cohort [2].
Clinical trial: Up to now, FRAX1036 is still in the preclinical development stage.
References:[1] Ong CC 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] Chow HY et al. Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget.2015 Feb 10;6(4):1981-94.
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免疫组化多聚物法
immunohistochemistry
英[ɪmjʊnəʊhɪstəʊ'kemɪstrɪ]
美[ɪmjʊnoʊhɪstoʊ'kemɪstrɪ]
[词典]免疫组织化学;
[例句]Methods Transmission electron microscope and immunohistochemistry were used.
方法采用透射电镜和免疫组化法。
英 [ˈpɒlɪmə(r)]
美 [ˈpɑ:lɪmə(r)]
n.
多聚物; [高分子] 聚合物;
[例句]The nature of the polymer is currently a trade secret.
这一聚合物的性质目前是个商业机密。
[其他]
复数:polymers
高分子化合物又称高分子(聚合物),高分子是由分子量很大的长链分子所组成,高分子的分子量从几千到几十万甚至几百万。而每个分子链都是由共价键联合的成百上千的一种或多种小分子构造而成。高分子的分类有多种,按来源可分为天然高分子、天然高分子衍生物、合成高分子三大类;根据用途则可分为合成树脂和塑料、合成橡胶、合成纤维等;按热行为可分为热塑性和热固性聚合物;按主链结构可分为碳链、杂链、和元素有机三类;另外根据工业产量和价格还可分为通用高分子、中间高分子、工程塑料以及特种高分子等等。
苏州高分子科学先进材料有限公司
polymer英[ˈpɒlɪmə(r)]美[ˈpɑ:lɪmə(r)]
n.多聚物; [高分子] 聚合物;
[例句]The nature of the polymer is currently a trade secret.
这一聚合物的性质目前是个商业机密。
[其他]复数:polymers
Author:AndrewJ.Hall,MilenaQuaglia,PanagiotisManesiotis,ErsiliaDeLorenzi,andBörjeSellergren
Resource:AnalyticalChemistry,2006,78(24):8362-8367.
Abstract:
Arangeof2-acrylamidopyridines,showingsubtledifferencesinsolutionbindingtowardcarboxylicacids,hasbeeninvestigatedasfunctionalmonomersinmolecularimprinting.ImprintingofN-Z-L-glutamicacidwithonesuchmonomerisshowntobeeffectiveinthecreationofamolecularlyimprintedpolymer(MIP)withrecognitionpropertiesforitstemplateandalsoforlargermoleculescontainingglutamicacidresidues.IncomparisontoaMIPpreparedviaamore"trADItional"approach,thenewpolymericreceptorsexhibitreducednonspecificbinding.Thenewreceptorsarecomparedwithpreviouslyreportedurea-basedreceptorstargetingtheglutamicacidresidueandreceptorstargetingthepteridinesubstructureoffolicacid.
PMID:17165828

