ProductDescription
GDC0879ishighlyselective,orally-bioavailable,oxime-containingpyrazoletypeinhibitorofB-Raf(V600E)kinasewithapotencyof0.13nM.[1]Inascreeningofapanelofkinasesat1uMactivityonlyRAFkinaseswereshowntohave>90%inhibition,withonlyoneadditionalkinase(caseinkinase1-delta)at>50%inhibition.[2]GDC0879effectivelyreducespERKlevelsat63nMandcellularviABIlityofB-RafmutantMALME3Mcellsat0.75uM.[2]
InA375melanomaandColo205colorectalcarcinomacelllines,GDC0879exhibitsdose-depdnentpMEK1inhibitionof59and29nM,respectively.Noevidenceofapoptoticactivationpathwaysinvitrowasobserved,suggestingthatGDC0879"santitumoractivityisbasedprimarilyonitseffectoncellproflieration.[1]PathwaymodulationinA375tumorswasshowntobesignificant(13%and28%activityremainingat1and4hours,respectively)bymeasuringMEK1phoshporylationofSer217/221.ReducedlevelsofpMEK1werestillevidentat8hpostdose(59%),butreturnedtobaselineat12h.SimilarstudiesinSK23tumorsdidnotdisplaysuchastrongPDeffect.
Technicalinformation:
| ChemicalFormula: | C19H18N4O2 | |
| CAS#: | 905281-76-7 | |
| MolecularWeight: | 334.37 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | (E)-5-(1-(2-hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydroinden-1-oneoxime | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | GDC-0879,GDC0879,GDC0879 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Wongetal.,Pharmacodynamicsof2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol(GDC-0879),apotentandselectiveB-Rafkinaseinhibitor:understandingrelationshipsbetweensystemicconcentrations,phosphorylatedmitogen-activatedproteinkinasekinase1inhibition,andefficacy.J.Pharm.Exp.Ther.2009,329(1),360-367PubmedID:19147858 |
| 2. | Hoeflichetal.,AntitumorefficacyofthenovelRAFinhibitorGDC-0879ispredictedbyBRAFV600Emutationalstatusandsustainedextracellularsignal-regulatedkinase/mitogen-activatedproteinkinasepathwaysuppression.CancerRes.2009,69(7),3042-3051PubmedID:19276360 |
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。
