ProductDescription
PF-04217903isatriazolopyrazine-based,ATP-competitiveinhibitorofc-MetwithKiandcellularIC50potencyof4nMand5nM,respectively.[1]Inabroadpanellofover200kinases,PF-04217903showed>1000-foldselectivityforc-Met.Forc-Metmutations,PF-04217903exhibitedactivitiesof6.4nM,6.7nM,and3.1nMforendogenousc-Met-R988C,endogenousC-Met-T1010I,andentineeredc-Met-H1094R,respectively.[3]
Additionally,PF-04217903inhibitedproliferation,cellsurvival,migration/invasioninMET-amplifiedcelllinesinvitroandwasefficaciousintumormodelswitheitherMETgeneamplificationorhepatocytegrowthfactor(HGF)/c-Metautocrineloopinvivo.[2,4]Efficacywasdose-dependentandcorrelatedwithinhibitionofc-Metphosphorylationanddownstreamsignaling.
Duetoitsexquisiteselectivityprofile,PF-04217903canbeconsideredasapowerfultoolinprobingc-Metcatalyticactivityinpreclinicalmodelsforcancerprogression.
Technicalinformation:
| ChemicalFormula: | C20H20N8O4S | |
| CAS#: | 956906-93-7 | |
| MolecularWeight: | 468.49 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 2-(4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-1H-pyrazol-1-yl)ethanolmesylate | |
| Solubility: | Upto15mMinDMSO | |
| Synonyms: | PF-04217903,PF04217903,PF04217903 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Cuietal.,Discoveryofanovelclassofexquisitelyselectivemesenchymal-epithelialtransitionfactor(c-MET)proteinkinaseinhibitorsandidentificationoftheclinicalcandidate2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol(PF-04217903)forthetreatmentofcancer.J.Med.Chem.2012,55,8091-8109.PubmedID:22924734 |
| 2. | Zouetal.,SensitivityofselectedhumantumormodelstoPF-04217903,anovelselectivec-Metkinaseinhibitor.Mol.CancerTher.2012,11,1036-1047.PubmedID:22389468 |
| 3. | Timofeevskietal.,Enzymaticcharacterizationofc-Metreceptortyrosinekinaseoncogenicmutantsandkineticstudieswithaminopyridineandtriazolopyrazineinhibitors.Biochemistry,2009,48,5339-5349.PubmedID:19459657 |
| 4. | Shojaeietal.,HGF/c-Metactsasanalternativeangiogenicpathwayinsunitinib-resistanttumors.CancerRes.2010,70,10090-10100.PubmedID:22389468 |
Cellagen的ChamQ SYBR qPCR预混液（无ROX）| Q321产品描述ChamQSYBR®qPCR预混液（Vazyme，＃Q321）由香槟Taq DNA聚合酶（Vazyme，＃P122）通过抗体修饰的热启动激活技术保护，是专为基于SYBR Green I的定量PCR（qPCR）设计的。ChamQSYBR®qPCR Master Mix的优化缓冲液系统中的独特因素（即促进特异性的Exactor）大大提高了其灵敏度和特异性。该混合物以2倍反应浓度制备，可直接用于鲁棒性低模板qPCR，具有高灵敏度，特异性和可靠性。优点特异性+敏感性的最佳组合。独特的抗体修饰的热启动taq，具有独特的特异性促进因子。Mg2 +和染料的最佳浓度。
