SB-431542isapotentandselectiveinhibitorofALK5andALK4withIC₅₀valuesof94nMand14nM,respectivelly,andisalsoaninhibitorofTGF-βReceptor.

IC50:94nM(ALK5),140nM(ALK4)

SB-431542(1μM)significantlyreducestheTGF-β-inducednuclearaccumulationofSmadproteinsinA498cells.SB-431542inhibitsTGF-β1-inducedcollagenIα1andPAI-1mRNAwithIC₅₀valuesof60and50nM,respectively.Inaddition,SB-431542inhibitsTGF-β1-inducedfibronectinmRNAandproteinwithIC₅₀valuesof62and22nM,respectively^[1].SB-431542(10μM)isaselectiveinhibitorofendogenousactivinandTGF-βsignalingbuthasnoeffectonBMPsignalinginNIH3T3cells^[2].TRKI,SB-431542,inhibitsTGF-beta-inducedtranscription,geneexpression,apoptosis,andgrowthsuppression.SB-431542attenuatesthetumor-promotingeffectsofTGF-beta,includingTGF-beta-inducedEMT,cellmotility,migrationandinvasion,andvascularendothelialgrowthfactorsecretioninhumancancercelllines.SB-431542inducesanchorageindependentgrowthofcellsthataregrowth-inhibitedbyTGF-beta,whereasitreducescolonyformationbycellsthataregrowth-promotedbyTGF-beta^[3].SB-431542(0.3μM)inhibitscellproliferationinducedbyTGF-βinMG63cells^[4].

SB-431542(10mg/kg,i.p.)decreaseslungmetastasisbutdoesnotsignificantlyaltergrowthoftheprimarytumor4T1xenograft^[5].

• [1].N.J.Laping,etal.InhibitionofTransformingGrowthFactor(TGF)-β1-InducedExtracellularMatrixwithaNovelInhibitoroftheTGF-βTypeIReceptorKinaseActivity:SB-431542.

  [2].InmanGJ,etal.SB-431542isapotentandspecificinhibitoroftransforminggrowthfactor-betasuperfamilytypeIactivinreceptor-likekinase(ALK)receptorsALK4,ALK5,andALK7.MolPharmacol,2002,62(1),65-74.

  [3].HalderSK,etal.AspecificinhibitorofTGF-betareceptorkinase,SB-431542,asapotentantitumoragentforhumancancers.Neoplasia,2005,7(5),509-521.

  [4].MatsuyamaS,etal.SB-431542andGleevecinhibittransforminggrowthfactor-beta-inducedproliferationofhumanosteosarcomacells.CancerRes,2003,63(22),7791-7798.

  [5].SatoM,etal.DifferentialProteomeAnalysisIdentifiesTGF-β-RelatedPro-MetastaticProteinsina4T1MurineBreastCancerModel.PLoSOne.2015May18;10(5):e0126483.

Atotalof100,000cellsfromeachpoolofA549andHT29areseededintoeachwellof12-wellplate.Cellsareculturedinmediacontaining0.2%FBSfor18hours,andthentreatedwith5ng/mLTGF-β1inthepresenceofSB-431542(10µM)in0.5mLofmediafor24hours.OnehundredμLsofeachsupernatantmediaisusedforVEGFassayaccordingtothemanufacturer"sinstruction.ForTGF-β1ELISA,100,000cellsfromeachpoolofA549,VMRC-LCD,andHT29areseededintoeachwellof12-wellplatesandserum-starvedfor20hours.CellsarethentreatedwithSB-431542in0.5mLofserum-freeRPMImediafor24hours.OnehundredμLsofeachsupernatantmediaisactivatedandusedforTGF-β1assayaccordingtothemanufacturer"sinstruction.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

SB-431542isdissolvedataconcentrationof10mMinDMSO.

A498cellsareseededat5,000to10,000cells/wellin96-wellplates.Thecellsareserum-deprivedfor24handthentreatedwithSB-431542for48htoassessthecellulartoxicity.CellviABIlityisdeterminedbyincubatingcellsfor4hwithXTTlabelingandelectroncouplingreagentaccordingtothemanufacturer"sdirections.Livecellswithactivemitochondriaproduceanorange-coloredproduct,formazan,whichisdetectedusingaplatereaderatbetween A 450nm andA 500nm withareferencewavelengthgreaterthan600nm.Theabsorbancevaluescorrelatewiththenumberofviablecells.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

SB-431542isformulatedin20%DMSO/80%cornoil.

Tenthousand4T1cellsareinjectedsubcutaneouslyintothesecondmammaryfatpadof6-week-oldBalb/cfemalemice.Tumorsaremeasuredtwiceweekly,andvolumeiscalculatedusingthefollowingformula:Volume=width²×length×0.52.Micearerandomlyassignedtotwotreatmentgroups:control,n=14(20%DMSO/80%cornoil);SB-431542-treated,n=15(10mg/kgbodyweightin20%DMSO/80%cornoil,administeredintraperitoneallythreetimesperweekstartingonedayaftertumorcellinoculation.Primarytumorsareresectedwhenthevolumeatday10post-injectionof4T1cells.Allmicearemonitoreddailyandeuthanizedafter4weeks.Themetastasesaredissectedtosnap-freezeforfurtheranalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].N.J.Laping,etal.InhibitionofTransformingGrowthFactor(TGF)-β1-InducedExtracellularMatrixwithaNovelInhibitoroftheTGF-βTypeIReceptorKinaseActivity:SB-431542.

  [2].InmanGJ,etal.SB-431542isapotentandspecificinhibitoroftransforminggrowthfactor-betasuperfamilytypeIactivinreceptor-likekinase(ALK)receptorsALK4,ALK5,andALK7.MolPharmacol,2002,62(1),65-74.

  [3].HalderSK,etal.AspecificinhibitorofTGF-betareceptorkinase,SB-431542,asapotentantitumoragentforhumancancers.Neoplasia,2005,7(5),509-521.

  [4].MatsuyamaS,etal.SB-431542andGleevecinhibittransforminggrowthfactor-beta-inducedproliferationofhumanosteosarcomacells.CancerRes,2003,63(22),7791-7798.

  [5].SatoM,etal.DifferentialProteomeAnalysisIdentifiesTGF-β-RelatedPro-MetastaticProteinsina4T1MurineBreastCancerModel.PLoSOne.2015May18;10(5):e0126483.

384.39

C₂₂H₁₆N₄O₃

301836-41-9

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥40mg/mL;Ethanol:11.17mg/mL(Needultrasonicandwarming)

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.24%

SelectBatch:HY-10431-16278HY-10431-04750HY-10431-12188

DataSheet(125KB)SDS(120KB)

COA(95KB)HNMR(204KB)LCMS(237KB)

HandlingInstructions(1252KB)

• [1].N.J.Laping,etal.InhibitionofTransformingGrowthFactor(TGF)-β1-InducedExtracellularMatrixwithaNovelInhibitoroftheTGF-βTypeIReceptorKinaseActivity:SB-431542.

  [2].InmanGJ,etal.SB-431542isapotentandspecificinhibitoroftransforminggrowthfactor-betasuperfamilytypeIactivinreceptor-likekinase(ALK)receptorsALK4,ALK5,andALK7.MolPharmacol,2002,62(1),65-74.

  [3].HalderSK,etal.AspecificinhibitorofTGF-betareceptorkinase,SB-431542,asapotentantitumoragentforhumancancers.Neoplasia,2005,7(5),509-521.

  [4].MatsuyamaS,etal.SB-431542andGleevecinhibittransforminggrowthfactor-beta-inducedproliferationofhumanosteosarcomacells.CancerRes,2003,63(22),7791-7798.

  [5].SatoM,etal.DifferentialProteomeAnalysisIdentifiesTGF-β-RelatedPro-MetastaticProteinsina4T1MurineBreastCancerModel.PLoSOne.2015May18;10(5):e0126483.

品牌介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

品牌分类

黄酮类化合物 抑制性抗体 苯丙素类 酸和醛 醌类 肽 其他 酚类 萜类和糖苷类

类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

显示分类

联络我们

服务热线：4000-520-616

（限工作日9:00-18:00）

QQ ：1570468124

手机：18915418616

官网：http://www.medchemexpress.com/

快速导航：

公司介绍

产品中心

新闻动态

在线咨询

联系我们

公司介绍

产品中心

新闻动态

在线咨询

联系我们

总部地址：

江苏省苏州市工业园区星湖街218号 苏州生物医药产业园一期（生物纳米园）A4-216(邮编：215125)

工作时间：周一至周五9:00~18:00

技术支持：

Email：info@ebiomall.com

短信：18915418616

服务热线：

4000-520-616（全国）

☏  0512-67156496（苏州）

版权信息：

©  2015-2022 苏州蚂蚁淘生物科技有限公司 版权所有 中国

网站备案：

苏ICP备17049038号-1

苏公网安备 32059002001627号

友情链接：

联系QQ:764052152

medix官网 medkoo代购 megazyme清关 microspheres正品 midlandsci采购 minerva报价 molecular molinnov moltox mpbio RevMAb中国 ​​polysciences药物筛选 enogene公司 Viskase Corporation apolloAPI华东代理 美国Novus Immunology Consultan 蚂蚁淘 广东海达仪器制造有限公司

免责声明：

本站有部分内容来自互联网，如无意中侵犯了某个媒体 、公司 、企业或个人等的知识产权，请来电或致函告之，
本网站将在规定时间内给予删除等相关处理。

扫描二维码关注官方微信

获取最新促销及产品信息