LC Labs/M-2900 Motesanib, Free Base, 99%/M-2900/500 mg
市场价：
¥17200.00
美元价：
10320.00
产品分类：
其他试剂
公司分类：
Other_reagents
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
- Motesanib,alsoknownasAMG-706,isanorallyadmiNISTeredmultikinaseinhibitorthatselectivelytargetsVEGFreceptors,platelet-derivedgrowthfactorreceptors,andKitreceptorswithIC50valuesof2nM(VEGFR1),3nM(VEGFR2),6nM(VEGFR3),84nM(PDGFR),and8nM(Kit).Itinhibitsangiogenesisandtumorgrowthintumorxenografts.Polverino, A.et al.,“AMG706,anoral,multikinaseinhibitorthatselectivelytargetsvascularendothelialgrowthfactor,platelet-derivedgrowthfactor,andkitreceptors,potentlyinhibitsangiogenesisandinducesregressionintumorxenografts.”Cancer Res. 66: 8715‑8721 (2006).
- HumanbreastcancerxenograftmodelswereestablishedinathymicnudemicebyimplantingMCF-7(luminal),MDA-MB-231(mesenchymal)tumorfragments,orCal-51(mixed/Progenitor)tumorcells.Motesanibtreatmentsignificantlyinhibitedthetumorgrowthdose-dependentlyandreducedviabletumorfractionandbloodvesseldensityinvivo.However,motesanibdidnotaffecttheproliferationoftumorcellsinvitro.Coxon, A.et al.,“Broadantitumoractivityinbreastcancerxenograftsbymotesanib,ahighlyselective,oralinhibitorofvascularendothelialgrowthfactor,platelet-derivedgrowthfactor,andKitreceptors.”Clin. Cancer Res. 15: 110‑118 (2009).
- MotesanibinhibitedmutatedKitkinaseautophosphorylation.Italsosuppressedkinasedomainmutationsconferringimatinibresistancebutdidnotinhibittheimatinib-resistantD816Vmutant.MotesanibinhibitedtheproliferationofBa/F3cellsexpressingKitmutants.Caenepeel, S.et al.,“MotesanibinhibitsKitmutationsassociatedwithgastrointestinalstromaltumors.”J. Exp. Clin. Cancer Res. 29: 96 (2010).
- MotesanibdemonstratedsomeantitumoractivityinaPhaseIstudy.Rosen, L.S.et al.,“Safety,pharmacokinetics,andefficacyofAMG706,anoralmultikinaseinhibitor,inpatientswithadvancedsolidtumors.”J. Clin. Oncol. 25: 2369‑2376 (2007).
- Motesanibinhibitedthyroidtumorxenograftgrowth,possIBLybyinhibitionofangiogenesisandexpressionofVEGFR2andRetontumorcells.Coxon, A.et al.,“AntitumorActivityofMotesanibinaMedullaryThyroidCancerModel.”J. Endocrinol. Invest. (Mar 21,2011-Epub ahead of print).
- InaphaseIIstudy,93patientswhohadprogressive,locallyadvancedormetastatic,rADIoiodine-resistantdifferentiatedthyroidcancerweretreatedwithmotesanibdiphosphate.Motesanibdiphosphateinducedpartialresponsesinthesepatients.Anticancerresponsesweredemonstratedin14%ofpatients.DiseasestABIlizationwasshownin67%ofpatients.Sherman, S.I.et al.,“Motesanibdiphosphateinprogressivedifferentiatedthyroidcancer.”N. Engl. J. Med. 359: 31‑42 (2008).
- AnotherCASnumberpreviouslyassignedtomotesanibfreebase,namely894356-47-9,hasbeendeletedbyCASandisnolongerinuse.
- Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.
- ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanadianpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
- Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.
C22H23N5O
[453562-69-1]
M.I.14:10338
Storage
Storeatorbelow-20ºCSolubility
SolubleinDMSOat200mg/mL;solubleinethanolat40mg/mL;verypoorlysolubleinwater;maximumsolubilityinplainwaterisestimatedtobeabout50-100µM;buffers,serum,orotheradditivesmayincreaseordecreasetheaqueoussolubility品牌介绍
LC Laboratories 公司提供信号转导，调节蛋白亚细胞定位试剂（抗生素）产品蛋白抑制剂产品。LC Laboratories（LC Labs）公司成立于1980年，一直专注于信号转导，肿瘤以及其他临床前试剂的研究和生产，主要提供抗癌物质、酶抑制剂、激活剂和离子通道试剂。LC Labs公司不但拥有大规模的制备液相色谱纯化能力，也开发和优化了大量的具有自主知识产权的低成本高纯度生成方法，其生产的小分子试剂纯度高、价格低和销量大。1980年，LC Labs是PMA（佛波醇12-豆蔻酸 13醋酸；TPA）的全球主要生产商，36年来的销售量超过150,000瓶；1989年为研究试剂市场提供第一个纯度高价格低的毒萝卜素；1990年提供第一个纯度高价格低的冈田酸；1991年提供第一个纯度高价格低的花萼海绵诱癌素A，并且持续是这种广泛使用的磷酸酶抑制剂的全球主要生产商；1995年提供第一个异构体级别纯度的低价格Gö 6976；1996年提供第一个纯度高价格低的罗霉素A1；2002年提供第一个纯度高价格低的雷帕霉素（抗真菌抗生素）；同年，提供第一个纯度高、价格低的FK-506；2003年提供第一个纯度高价格低的来普霉素B；2004年提供第一个纯度高价格低的星孢菌素；同年，提供第一个纯度高价格低的环巴胺；2007年，LC Labs公司为临床前肿瘤相关研究引入第一组纯度高价格低的常用蛋白激酶抑制剂。
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