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Description | RapamycinisaspecificmTORinhibitorwithIC50of0.1nM. |
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IC50&Target | IC50:0.1nM(mTOR)[1] |
InVitro | RapamycininhibitsendogenousmTORactivityinHEK293cellswithIC50of0.1nM,morepotentlythaniRapandAP21967withIC50of5nMand10nM,respectively[1].RapamycinexertsitsantitumoreffectonmalignantgliomacellsbyinducingautophagyandsuggestthatinmalignantgliomacellsadisruptionofthePI3K/AktsignalingpathwaycouldgreatlyenhancetheeffectivenessofmTORinhibitors.RapamycininhibitscellviABIlityinallthreecelllinesinadose-dependentmanner,buttheirsensitivitiesvaried.TheIC50levelsofT98G,U87-MG,andU373-MGcellsare2nM,1μM,and>25μM,respectively[3]. |
InVivo | TreatmentwithRapamycin(i.p,1.5mg/kg)almostcompletelypreventsthehypertrophicincreasesinplantarismuscleweightandfibresizeat7and14days[4].WTorLS/+micearetreateddailyRapamycin(2mg/kgbodyweighti.p.)for4weeks,followsbyanadditional4weeksofweeklyinjectionsofthesamedose.ThereissignificantreversaloftheabnormalfetalgeneexpressionprofileofheartsfromRapamycin-treatedLS/+mice[5]. |
ClinicalTrial | ViewMoreCollapse |
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PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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KinaseAssay [1] | HEK293cellsareplatedat2-2.5×105cellsperwellofa12-wellplateandserum-starvedfor24hinDMEMonly.Cellsaremock-treatedortreatedwithRapamycin(0.05-50nM),iRap(0.5-500nM),orAP21967(0.5-500nM)for15minutesat37°C.Serumisaddedtoafinalconcentrationof20%for30minutesat37°C.CellsarelysedandcelllysatesareseparatedbySDS-PAGE.ResolvedproteinsaretransferredtoaPVDFmembraneandimmunoblottedwithaphosphospecificprimaryantibodyagainstThr389ofp70S6kinase.DataareanalyzedusingImageQuantandKaleidaGraph[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
CellAssay [2] | RapamycinisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[2]. HL-60,NB4,U937,KG-1,andK562cellsarepassagedroutinelyinRPMI-1640supplementedwith10%heat-inactivatedFBS,2mML-glutamine,50U/mLpenicillinand50μg/mLstreptomycinina5%CO2humidifiedatmosphereat37°C.Fortheexperiments,exponentiallygrowingcellsareharvestedbycentrifugation,andresUSPendedinfreshmediumcontaining10%FBS.Thecellsareseededataninitialcelldensityof2×105/mLinBDFalconsix-wellplatesinthepresenceofvariousconcentrationsofDMSOor1μMATRA.Rapamycin(20nM)isadded20minpriortothedifferentiationagents.Atday2,0.3mLoffreshmediumisaddedtoeachwell.Theviablecellsaredeterminedbytrypanblueexclusionandquantifiedusingahemocytometer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
AnimalAdmiNISTration [4][5] | Rapamycinisdissolvedin2%carboxymethylcellulose(Rat)[4]. Rat[4] | ||||||||||||||||
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MolecularWeight | 914.17 | ||||||||||||
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Formula | C₅₁H₇₉NO₁₃ | ||||||||||||
CASNo. | 53123-88-9 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | DMSO:≥28mg/mL Rapamycinispreparedinvehicle(16%DMSOin0.5w/v%methylcellulose400)[6]. *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> | ||||||||||||
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Purity:98.98%
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westblot蛋白免疫印迹实验跑小分子蛋白(15kd)条带一直是波浪状,有人说是胶的问题,可同时跑了36kd蛋白,条带是直的,有人说是要恒流跑,电压不要太大,我的转膜条件是50v,50min,请教各位大神指点,万分感谢!!!
如题,之前没做过药代,老师给了一个600+Da的五肽,想测下药代动参数,看文献推荐上述两种方法,但是不知道选哪种更好,lcms前处理会不会影响小肽。
求助各位前辈,我最近在合成的化合物水溶性很好,非常好,以至于可以随便溶解在水里,它的六氟磷酸盐也可以随意溶解在水里(大于50uM),细胞成像实验显示它根本进不去细胞,求问有没有啥方法包裹一下让它进去?我搜了一下文献,感觉多数是把脂溶性特别好的东西包裹一下弄进去的,也许是搜索姿势不对没找到我需要的答案,**点拨啊!!!
求助各位大神,现在想购买小分子数据库,求大神推荐。
我知道的免费的数据库有zinc
求推荐哪家公司或者研究所的小分子数据库可以购买,十分感谢!!!!!!
有机的是有机化合物的简称,它指的是含碳化合物.
但是,有四大类常见物质一般不作为有机物处理:
1、碳的氧化物,如CO和CO2.
2、碳酸及其盐,如CaCO3.
3、金属碳化物,如CaC2.
4、拟卤素及其化合物,如(CN)2与KSCN.
水的化学式为H2O,它不含有碳元素,故不是有机物.
但若所描述的水不是化学意义的水,而是自然界存在的天然水,那么,水中会溶有一定量的有机物.
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