Inavolisib-GDC-0077-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEInavolisibCat.No.:HY-101562CASNo.:2060571-02-8Synonyms:GDC-0077;RG6114分⼦式:C₁₈H₁₉F₂N₅O₄分⼦量:407.37作⽤靶点:PI3K;Apoptosis作⽤通路:PI3K/Akt/mTOR;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:110mg/mL(270.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4548mL12.2739mL24.5477mL5mM0.4910mL2.4548mL4.9095mL10mM0.2455mL1.2274mL2.4548mL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：1%DMSO>>99%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥0.55mg/mL(1.35mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.11mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.11mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.75mg/mL(6.75mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(6.75mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GDC-0077(RG6114)⼀种有效的，⼝服的选择性PI3Kα抑制剂(IC50=0.038nM)。GDC-0077(RG6114)通过与PI3K的ATP结合位点结合⽽发挥其活性，从⽽抑制了PIP2到PIP3的磷酸化。与野⽣型PI3Kα相⽐，GDC-0077(RG6114)对突变体的选择性更⾼[1]。IC50&TargetPI3Kα0.038nM(IC50)体外研究GDC-0077(RG6114)is>300-foldmoreselectiveforPI3KαovertheotherclassIPI3Kisoforms(β,δ,andγ)and>2000-foldmoreselectiveoverPIKfamilymembers.GDC-0077selectivelydegradesmutantPI3Kαinaproteasome-dependentfashionresultinginreductionofPI3KpathwayactivitybiomarkerssuchaspAKTandpPRAS40,inhibitionofcellproliferation,andincreasedapoptosisinhumanPIK3CA-mutantbreastcancercelllinestoagreaterextentwhencomparedtoPIK3CAwild-typecells[1].体内研究GDC-0077(p.o.)resultsintumorregressions,inductionofapoptosis,andareductionofpAKT,pPRAS40,andpS6RPinadose-dependentfashioninpatient-derivedPIK3CA-mutantbreastcancerxenograftmodels[1].户使⽤本产品发表的科研⽂献•ClinTranslMed.2022May;12(5):e835.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RHong,AbstractPD4-14:GDC-0077isaselectivePI3KalphainhibitorthatdemonstratesrobustefficacyinPIK3CAmutantbreastcancermodelsasasingleagentandincombinationwithstandardofcaretherapies.2017SanAntonioBreastCancerSymposium.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl