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FRAX1036p21-activated kinase I (PAK1) inhibitor |
Sample solution is provided at 25 µL, 10mM.
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Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
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。
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
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
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