WF-47-JS03-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEWF-47-JS03Cat.No.:HY-133551分⼦式:C₃₀H₃₈N₆O₂分⼦量:514.66作⽤靶点:RET作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(121.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9430mL9.7152mL19.4303mL5mM0.3886mL1.9430mL3.8861mL10mM0.1943mL0.9715mL1.9430mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.04mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.04mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性WF-47-JS03⼀种有效的选择性RET激酶抑制剂，⽐对激酶插⼊域受体(KDR)的选择性⾼500多倍。WF-47-JS03作⽤于转染KIF5B-RET的Ba/F3细胞和转染CCDC6-RET的LC-2/ad肺癌细胞，IC50分别为1.7nM和5.3nM。可透过⾎脑屏障[1]。体外研究WF-47-JS03inhibitsTel-KDRtransfectedBa/F3cellsandBa/F3wild-typecelllineswithIC50sof0.99and1.5μM,respectively[1].体内研究WF-47-JS03significantlyinhibitstumorgrowthinRIEKIF5B-RETxenograftmiceandiswelltoleratedat1,3,and10mg/kginthe10daystudy[1].AnimalModel:Female6-8weekoldHarlanFoxn1nudemicewithRIE-RET-KIF5BtransgeniccelllineDosage:1,3,10mg/kgAdministration:Dosedorally,1xdailyfor10daysResult:InhibitedtumorgrowthinRIEKIF5B-RETxenograftmice.REFERENCES[1].CaseyJNMathison,etal.EfficacyandTolerabilityofPyrazolo[1,5-a]pyrimidineRETKinaseInhibitorsfortheTreatmentofLungAdenocarcinoma.ACSMedChemLett.2020Feb12;11(4):558-565.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400