Technical Documents
Description
Details
Usage
- Coupling: 3 minute coupling time recommended.
- Deprotection: Ammonium hydroxide for 2 hours at 55°C or as required by nucleobases.|TIPS removal: After deprotection, dry down oligo and take up in 0.5 mL DMF.Add 0.1 mL TBAF. Vortex and keep at 45°C for 15 minutes.Quench with 0.5 mL 2 M TEAA and desalt on Glen Gel-Pak™ column or equivalent.
| Specifications | |
|---|---|
| Diluent | Anhydrous Acetonitrile |
| Storage | Freezer storage, -10 to -30�C, dry |
| Stability | 1-2 days |
Intellectual Property
Dilution/Coupling Data
The table below show pack size data and, for solutions, dilution and approximate coupling based on normal priming procedures.
ABI 392/394
| Catalog # | Pack Size | Grams/Pack | 0.1M Dil. (mL) | Approximate Number of Additions | |||||
|---|---|---|---|---|---|---|---|---|---|
| LV40 | LV200 | 40nm | 0.2μm | 1μm | 10μm | ||||
| 10-1544-02 | 0.25 g | .25grams | 2.52 | 70.67 | 42.4 | 26.5 | 19.27 | 14.13 | 3.53 |
| 10-1544-90 | 100 µmol | .099grams | 1 | 20 | 12 | 7.5 | 5.45 | 4 | 1 |
| 10-1544-95 | 50 µmol | .05grams | 0.5 | 3.33 | 2 | 1.25 | 0.91 | 0.67 | 0.17 |
Expedite
| Catalog # | Pack Size | Grams/Pack | Dilution (mL) | Approximate Number of Additions | ||||
|---|---|---|---|---|---|---|---|---|
| Molarity | 50nm | 0.2μm | 1μm | 15μm | ||||
| 10-1544-02 | 0.25 g | .25grams | 3.76 | 0.07 | 68.8 | 43 | 31.27 | 4.3 |
| 10-1544-90 | 100 µmol | .099grams | 1.5 | 0.07 | 23.6 | 14.75 | 10.73 | 1.48 |
| 10-1544-95 | 50 µmol | .05grams | 0.75 | 0.07 | 8.6 | 5.38 | 3.91 | 0.54 |
References
REFERENCE(S)| 1 C.W. Tornoe, C. Christensen, M. Meldal, J. Org. Chem. 2002, 67, 3057-3064; V. V. Rostovtsev, L. G. Green, V. V. Fokin, K. B. Sharpless, Angew. Chem. 2002, 114, 2708-2711; Angew. Chem. Int. Ed. 2002, 41, 2596-2599.| 2 C. J. Burrows, J. G. Muller, Chem. Rev. 1998, 98, 1109 â 1151.| 3 T. R. Chan, R. Hilgraf, K. B. Sharpless, V. V. Fokin, Org. Lett. 2004, 6, 2853 â 2855.| 4 J. Gierlich, G. A. Burley, P. M. E. Gramlich, D. M. Hammond, T. Carell, Org. Lett. 2006, 8, 3639-3642. F. Seela, V. R. Sirivolu, Chem. Biodiversity 2006, 3, 509-514.| 5 P. M. E. Gramlich, S. Warncke, J. Gierlich, T. Carell, Angew. Chem. 2008, 120, 3491â3493; Angew. Chem. Int. Ed. 2008, 47, 3442â 3444.| 6 P. M. E. Gramlich, C. T. Wirges, A. Manetto, T. Carell, Angew. Chem. Int. Ed. 2008, 47, 8350-8358.
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名称：氨氧基乙酸盐;羧甲氧基胺半盐酸盐；
分子式：C2H5NO3·0.5HCl
分子质量：109.30
熔点：156℃
【认领须知】
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ICML2017:PhaseIIIbMAGNIFYStudyofLenalidomideandRituximabCombinationinRelapsed/RefractoryFollicularandMarginalZoneLymphoma
AninterimanalysisofMAGNIFY,aphaseIIIb,randomized,open-label,multicenterstudyoftheR2combinationregimen(lenalidomide[Revlimid]plusrituximab[Rituxan])inpatientswithrelapsedorrefractorymarginalzonelymphoma,waspresentedattheInternationalConferenceonMalignantLymphoma(ICML)inLugano,Switzerland.ThisanalysisexpandedupondatapresentedearlierinthemonthattheASCOAnnualMeeting(Abstract7502).
TheMAGNIFYstudycontinuestoevaluatetheclinicalactivityof12cyclesofR2combinationtherapyfollowedbyrandomizationtoeither18cyclesofR2maintenanceor18cyclesofrituximabmonotherapy,inpatientswithrelapsedorrefractoryfollicularlymphoma,marginalzonelymphoma,ormantlecelllymphoma.Approximately500patientsareplannedtobeenrolledinthestudy.
Theprimaryendpointisprogression-freesurvival.Secondaryendpointsincludeoverallsurvival,overallresponserate,completeresponse,improvementofresponse,durationofresponse,durationofcompleteresponse,timetonextlymphomatreatment,timetohistologictransformation,safety,andexploratoryquality-of-lifemeasures.EnrollmentintheMAGNIFYstudyisongoing.
ASCOData
AttheASCOAnnualMeeting,interimdatawerepresentedfromananalysisofasubsetofpatientsfromtheMAGNIFYstudywithrelapsedorrefractoryfollicularlymphoma(n=160)withearly-relapse(n=52)anddouble-refractory(n=50)disease.
AttheJanuary9,2017,datacutoff,the1-yearprogression-freesurvivalforallfollicularlymphomapatientswas70%,with65%fordouble-refractorypatientsand49%forearly-relapsepatients.Additionally,evaluablefollicularlymphomapatients(n=128)hadanoverallresponserateof66%withacompleteresponse/completeresponse–unconfirmedrateof38%.Fordouble-refractorypatients(n=42),overallresponseratewas45%withacompleteresponse/completeresponse–unconfirmedrateof21%andforearly-relapsepatients(n=43),overallresponseratewas47%withacompleteresponse/completeresponse–unconfirmedrateof21%.Mediandurationofresponsewasnotmetatamedianfollow-upof10.2months.
Themostcommongrade3or4adverseeventsobservedinthestudyforallfollicularlymphoma,double-refractory,andearly-relapsepatients,respectively,wereneutropenia(29%,42%,37%),fatigue(6%,4%,8%),leukopenia(5%,8%,10%),thrombocytopenia(4%,8%,4%),andlymphopenia(3%,6%,4%).
ICMLData
DatapresentedatICMLinaseparateanalysisfocusedonpatientswithmarginalzonelymphoma(n=38),includingnodalmarginalzonelymphoma(n=18),splenicmarginalzonelymphoma(n=10),andmucosa-associatedlymphoidtissuelymphoma(n=10).
Atamedianfollow-upof13.8monthsfrominitiationoftherapywiththeR2combination,evaluablepatientswithmarginalzonelymphoma(n=32)achievedanoverallresponserateof66%withacompleteresponse/completeresponse–unconfirmedrateof44%.Evaluablenodalmarginalzonelymphomapatients(n=14)hadanoverallresponserateof57%withacompleteresponse/completeresponse–unconfirmedrateof57%.Evaluablesplenicmarginalzonelymphomapatients(n=8)hadanoverallresponserateof63%withacompleteresponserateof25%;andevaluablemucosa-associatedlymphoidtissuelymphomapatients(n=10)hadanoverallresponserateof80%withacompleteresponse/completeresponse–unconfirmedrateof40%.Mediandurationofresponsewasnotreachedforanygroup.
Themostcommongrade3or4adverseeventsobservedinpatientswithmarginalzonelymphomawereneutropenia(32%),thrombocytopenia(16%),andleukopenia(11%).
“Thechemotherapy-freecombinationoflenalidomideandrituximab,withcomplementarymechanismsofactionthatarethoughttoenhanceantibodydependentcellularcytotoxicity,continuestoshowencouragingactivityandatolerablesafetyprofileinindolentlymphomas,andparticularlyindifficult-to-treatpatientsubsets,”saidDavidJ.Andorsky,MD,co–principalinvestigatorofthestudyandmedicaloncologistattheRockyMountainCancerCentersinBoulder,Colorado.“Theseresultsinpatientswhohadfailedmultipletherapiesorrelapsedearly,aswellastheactivityinmarginalzonepatientsmeritfurtherstudyinthisareaofindolentlymphoma.”
AboutMAGNIFY
MAGNIFYisaphaseIIIb,multicenter,open-labelstudyofpatientswithgrades1–3bortransformedfollicularlymphoma,marginalzonelymphoma,ormantlecelllymphomawhoreceivedatleast1priortherapyandhadstageI–IV,measurabledisease.Approximately500patientsareplannedforenrollmentin12cyclesofR2induction,withaprojected314patientswithatleaststablediseaseafterinductionrandomized(1:1)to2maintenancearms.
Inductionincludesorallenalidomideat20mg/d,days1–21per28-daycycle(d1–21/28)plusintravenousrituximabat375mg/m2,days1,8,15,and22ofcycle1andday1ofcycles3,5,7,9,and11(28-daycycles).Patientsarethenrandomizedtomaintenancelenalidomideat10mg/d,days1to21/28,cycles13to30,plusrituximabat375mg/m2,day1ofcycles13,15,17,19,21,23,25,27,and29(R2,armA),orrituximabalone(sameschedule,armB).PatientsreceivingR2maintenanceafter18cyclesmaycontinuemaintenancelenalidomidemonotherapyat10mg/d,days1–21/28(perpatientand/orinvestigatordiscretion),untildiseaseprogressionastolerated.Patientswillbefollowedfor≥5yearsafterthelastpatientinitiatesinductiontherapy.
【认领须知】
1、认领翻译的战友请跟帖注明“认领本文翻译，48小时内未完成，请其他战友认领！”
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3、经常认领而不能及时提供优质稿件者将被列入黑名单，取消认领资格，请大家注意！
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FDAApprovesLenalidomideasMaintenanceTherapyforPatientsWithMultipleMyelomaFollowingAutologousStemCellTransplant
OnFebruary22,theU.S.FoodandDrugAdmiNISTration(FDA)expandedtheexistingindicationforlenalidomide(Revlimid)10mgcapsulestoincludeuseforpatientswithmultiplemyelomaasmaintenancetherapyfollowingautologoushematopoieticstemcelltransplant.TheexpandedindicationmakeslenalidomidethefirstandonlytreatmenttoreceiveFDAapprovalformaintenanceusefollowingautologoushematopoieticstemcelltransplant.
“Autologousstemcelltransplantafterinductiontherapyispartofthecontinuumofcarefortransplant-eligIBLe[patientswith]multiplemyeloma.However,mostpatientswillstillseetheirdiseaserecurorprogressafterthistreatment,”saidPhilipMcCarthy,MD,Director,BloodandMarrowTransplantCenter,DepartmentofMedicineatRoswellParkCancerInstitute.“Lenalidomidemaintenancetherapy,whichhasbeenshowntoincreaseprogression-freesurvivalfollowingautologousstemcelltransplantinclinicaltrials,canbeconsideredastandardofcareforthesepatients.”
ClinicalTrialFindings
Theapprovalwasbasedontwolargestudies—CALGB100104andIFM2005-02—includingmorethan1,000patientscomparinglenalidomidemaintenancetherapygivenuntildiseaseprogressionorunacceptabletoxicityafterautologoushematopoieticstemcelltransplantvsnomaintenance.Inbothstudies,theprimaryefficacyendpointwasprogression-freesurvival.
Inthemostcurrentprogression-freesurvivalanalysis,Study1(CALGB100104)demonstratedamedianprogression-freesurvivalof5.7years(95%confidenceinterval[CI]=4.4–notestimable)vs1.9years(95%CI=1.6–2.5)fornomaintenance,adifferenceof3.8years(hazardratio[HR]=0.38;95%CI=0.28–0.50).
Study2(IFM2005-02)alsoshowedabenefitwithamedianprogression-freesurvivalof3.9years(95%CI=3.3–4.7)vs2years(95%CI=1.8–2.3)fornomaintenance,adifferenceof1.9years(HR=0.53;95%CI=0.44–0.64).
Individualstudieswerenotpoweredforanoverallsurvivalendpoint.
AdescriptiveanalysisshowedthemedianoverallsurvivalinStudy1was9.3years(95%CI=8.5–notestimable)forpatientswhoreceivedlenalidomidevs7years(95%CI=5.9–8.6)fornomaintenance(HR=0.59;95%CI=0.4–0.78).InStudy2,medianoverallsurvivalwas8.8years(95%CI=7.4–notestimable)forpatientswhoreceivedlenalidomidevs7.3years(95%CI=6.7–9.0)fornomaintenance(HR=0.90;95%CI=0.72–1.13).
AdverseEvents
Themostfrequentlyreportedadversereactionsin≥20%(lenalidomidearm)acrossbothmaintenancestudies(Study1,Study2respectively)wereneutropenia(79%,61%);thrombocytopenia(72%,24%);leukopenia(23%,32%);anemia(21%,9%);upperrespiratorytractinfection(27%,11%);bronchitis(5%,47%);nasopharyngitis(2%,35%);cough(10%,27%);gastroenteritis(0%,23%);diarrhea(55%,39%);rash(32%,8%);fatigue(23%,11%);asthenia(0%,30%);musclespasm(0%,33%);andpyrexia(8%,21%).ThemostfrequentlyreportedGrade3or4reactions(morethan20%inthelenalidomidearm)includedneutropenia,thrombocytopenia,andleukopenia.
Thefrequenciesofonsetofadversereactionsweregenerallyhighestinthefirst6monthsoftreatmentandthenthefrequenciesdecreasedovertimeorremainedstablethroughouttreatment.
Inpatientsreceivinglenalidomidemaintenancetherapy,hematologicsecondprimarymalignanciesoccurredin7.5%ofpatientscomparedto3.3%inpatientsreceivingplacebo.Theincidenceofhematologicplussolidtumor(excludingsquamouscellcarcinomaandbasalcellcarcinoma)secondprimarymalignancieswas14.9%,comparedto8.8%inpatientsreceivingplacebowithamedianfollow-upof91.5months.Nonmelanomaskincancersecondprimarymalignancies,includingsquamouscellcarcinomaandbasalcellcarcinoma,occurredin3.9%ofpatientsreceivinglenalidomidemaintenance,comparedto2.6%intheplaceboarm.
如题，之前买的sigma的粉末，太贵。加培养基又不方便
