MedKooCat#:100470
Name:Imatinibmesylate
CAS#:220127-57-1(mesylate)
ChemicalFormula:C30H35N7O4S
ExactMass:
MolecularWeight:589.71
ElementalAnalysis:C,61.10;H,5.98;N,16.63;O,10.85;S,5.44
RelatedCAS#:220127-57-1(mesylate) 152459-95-5(freebase)
Synonym:CGP57148;CGP57148;CGP-57148;CGP57148B;CGP-57148B;CGP57148B;STI571;STI-571;STI571;Imatinibmesylate;USbrandname:Gleevec.Foreignbrandname:Glivec
IUPAC/ChemicalName:N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamidemethanesulfonate
InChiKey:YLMAHDNUQAMNNX-UHFFFAOYSA-N
InChiCode:InChI=1S/C29H31N7O.CH4O3S/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36;1-5(2,3)4/h4-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34);1H3,(H,2,3,4)
SMILESCode:O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4.CS(=O)(O)=O
TechnicalData
ViewCoA:currentbatch,lot#EOS41226
ViewQCdata,previousbatchmlot#LC40125
AdditionalInformation
Accordingtohttp://en.wikipedia.org/wiki/Imatinib,Imatinibwasdevelopedinthelate1990sbybiochemistNicholasLydon,aformerresearcherforNovartis,oncologistBrianDrukerofOregonHealthandScienceUniversity(OHSU),andCharlesSawyersofMemorialSloan-KetteringCancerCenter,wholedtheclinicaltrialsconfirmingitsefficacyinCML.ImportantcontributionstoitsdevelopmentwerealsomadebyCarloGambacorti-Passerini,aphysicianscientistatUniversityofMilanoBicoccainItaly,andJohnGoldman,ahematologistatHammersmithHospitalinLondon,UK.Imatinibwasdevelopedbyrationaldrugdesign.AfterthePhiladelphiachromosomemutationanddefectivebcr-ablproteinwerediscovered,theinvestigatorsscreenedchemicallibrariestofindadrugthatwouldinhibitthatprotein.Withhigh-throughputscreening,theyidentified2-phenylaminopyrimidine.Thisleadcompoundwasthentestedandmodifiedbytheintroductionofmethylandbenzamidegroupstogiveitenhancedbindingproperties,resultinginimatinib GleevecreceivedFDAapprovalinMay2001.OnthesamemonthitmadethecoverofTIMEmagazineasthe"magicbullet"tocurecancer.Druker,LydonandSawyersreceivedtheLasker-DeBakeyClinicalMedicalResearchAwardin2009for"convertingafatalcancerintoamanageablechroniccondition".
Imatinibisasmallmoleculekinaseinhibitor.Gleevecfilm-coatedtabletscontainimatinibmesylateequivalentto100mgor400mgofimatinibfreebase.Imatinibmesylateisawhitetooff-whitetobrownishoryellowishtingedcrystallinepowder.ItsmolecularformulaisC29H31N7O•CH4SO3anditsmolecularweightis589.7.Imatinibmesylateissolubleinaqueousbuffers≤pH5.5butisveryslightlysolubletoinsolubleinneutral/alkalineaqueousbuffers.Innon-aqueoussolvents,thedrugsubstanceisfreelysolubletoveryslightlysolubleindimethylsulfoxide,methanolandethanol,butisinsolubleinn-octanol,acetoneandacetonitrile.InactiveIngredients:colloidalsilicondioxide(NF);crospovidone(NF);hydroxypropylmethylcellulose(USP);magnesiumstearate(NF);andmicrocrystallinecellulose(NF).Tabletcoating:ferricoxide,red(NF);ferricoxide,yellow(NF);hydroxypropylmethylcellulose(USP);polyethyleneglycol(NF)andtalc(USP).
MechanismofAction
Imatinibmesylateisaprotein-tyrosinekinaseinhibitorthatinhibitsthebcr-abltyrosinekinase,theconstitutiveabnormaltyrosinekinasecreatedbythePhiladelphiachromosomeabnormalityinCML.Imatinibinhibitsproliferationandinducesapoptosisinbcr-ablpositivecelllinesaswellasfreshleukemiccellsfromPhiladelphiachromosomepositivechronicmyeloidleukemia.ImatinibinhibitscolonyformationinassaysusingexvivoperipheralbloodandbonemarrowsamplesfromCMLpatients.Invivo,imatinibinhibitstumorgrowthofbcr-abltransfectedmurinemyeloidcellsaswellasbcr-ablpositiveleukemialinesderivedfromCMLpatientsinblastcrisis. Imatinibisalsoaninhibitorofthereceptortyrosinekinasesforplatelet-derivedgrowthfactor(PDGF)andstemcellfactor(SCF),c-kit,andinhibitsPDGF-andSCF-mediatedcellularevents.Invitro,imatinibinhibitsproliferationandinducesapoptosisinGISTcells,whichexpressanactivatingc-kitmutation.
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MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(ResearchTrianglePark,简称RTP),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
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MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。 MedKoo是世界的抗癌化学试剂和激酶抑制剂供应商之一。我们制造,销售和分销用于肿瘤学研究的高质量抗癌小分子试剂。我们的使命是建立世界上全面的抗癌小分子集合。我们还为制药行业,医学研究组织和学术机构提供高质量的研究服务。我们致力于以具有竞争力的价格提供服务和分子。MedKoo是您可靠的药物发现和药物分子采购合作伙伴。 CRISPR-Cas9是近年兴起的用于靶向基因组特定位置,进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说,在CRISPR和Cas9的作用下,经由小RNA分子的引导,靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中,crRNA(CRISPR-derivedRNA)与tracrRNA(trans-activatingRNA)结合形成的复合物能特异性识别靶基因序列,并引导Cas9核酸内切酶在靶定位点剪切双链DNA,随后,细胞的非同源末端连接修复机制(NHEJ)重新连接断裂处的基因组DNA,并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA(Donor)通过同源重组(HR)整合进断裂处的基因组,从而达到对基因组DNA进行修饰的目的。
目前,CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物,包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫,也包含多种细菌和植物,甚至在人体上也有应用。
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2.NaHCO3,Ba(OH)3,H2SO4
3.HCL,NaAlO2,NaHSO4
4.Ca(OH)2,Na2CO3,BaCO3
谢谢了
要原因
C.MgCl2溶液和氨水D.盐酸和NaAlO2溶液
为什么
2.NaNO3FeCl3AgNO3
分别有什么现象?谢谢回答!
(1)优级纯试剂 亦称保证试剂,为一级品,纯度高,杂质极少,主要用于精密分析和科学研究,常以GR表示。
(2)分析纯试剂 亦称分析试剂,为二级品,纯度略低于优级纯,杂质含量略高于优级纯,适用于重要分析和一般性研究工作,常以AR表示。
(3)化学纯试剂 为三级品,纯度较分析纯差,但高于实验试剂,适用于工厂、学校一般性的分析工作,常以CP表示。
(4)实验试剂 为四级品,纯度比化学纯差,但比工业品纯度高,主要用于一般化学实验,不能用于分析工作,常以 LR表示。
以上按试剂纯度的分类法已在我国通用。根据化学工业部颁布的“化学试剂包装及标志”的规定,化学试剂的不同等级分别用各种不同的颜色来标志,见表1。
表1 我国化学试剂的等级及标志
暂无品牌问答