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蚂蚁淘在线 / 品牌中心 / MedKoo / MedKoo Biosciences/BAY1082439/205923/2g

MedKoo Biosciences/BAY1082439/205923/2g

价格
￥113000.00
货号：205923-2g
浏览量：113
品牌：MedKoo
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商品描述
BAY1082439isanorallybioavailableinhibitoroftheclassIphosphoinositide3-kinase(PI3K)alphaandbetaisoformswithpotentialantineoplasticactivity.PI3Kalpha/betainhibitorBAY1082439selectivelyinhibitsbothPI3Kalpha,includingmutatedformsofPIK3CA,andPI3KbetainthePI3K/Akt/mTORpathway,whichmayresultintumorcellapoptosisandgrowthinhibitioninPI3K-expressingand/orPTEN-driventumorcells.ByspecificallytargetingclassIPI3Kalphaandbeta,thisagentmaybemoreefficaciousandlesstoxicthanpanPI3Kinhibitors.

MedKooCat#:205923
Name:BAY1082439
CAS#:1375469-38-7
ChemicalFormula:C25H30N6O5
ExactMass:494.2278
MolecularWeight:494.552
ElementalAnalysis:C,60.72;H,6.11;N,16.99;O,16.18


Synonym:BAY10-82439;BAY10-82439;BAY-10-82439;BAY1082439;BAY1082439;BAY-1082439.

IUPAC/ChemicalName:(S)-N-(8-(2-hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide

InChiKey:JGNRMIWLBBNSMU-KRWDZBQOSA-N

InChiCode:InChI=1S/C25H30N6O5/c1-16-18(4-3-7-26-16)24(33)29-25-28-21-19(23-27-8-9-31(23)25)5-6-20(22(21)34-2)36-15-17(32)14-30-10-12-35-13-11-30/h4-7,17,32H,8-15H2,1-2H3,(H,28,29,33)/t17-/m0/s1

SMILESCode:C1=CC(OC[C@@H](O)CN2CCOCC2)=C(OC)C2N=C(NC(=O)C3=CC=CN=C3C)N3CCN=C3C1=2


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:
ViewCoA:currentbatch,Lot#B7B11C06

QCData:
ViewQCdata:currentbatch,Lot#B7B11C06

SafetyDataSheet(MSDS):
ViewMaterialSafetyDataSheet(MSDS)

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:
Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:
SolubleinDMSO,notinwater

ShelfLife:
>2yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:
0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:
293490


AdditionalInformation

BAY1082439isahighlyselectivePI3Kα/α-balancedinhibitor.BAY1082439representsanewtypeofPI3Kinhibitorwithuniquepharmacologicalandpharmacodynamicproperties.BAY1082439hasanIC50ratioof1:3inbiochemicalassaysofPI3Kα(4.9nM)vs.PI3Kα(15.0nM),and>1000-foldselectivityagainstmTORkinase.Invivo,BAY1082439showedclearadvantagesoverthestrongPI3KαinhibitorBAY80-6946inPTEN/PI3Kα-driventumormodels(e.g.,PC3andHEC-1B),whenthetwocompoundswerecomparedattheirMTDs.FurThermore,BAY1082439hasuniquepharmacokinetic(PK)propertieswithveryhighplasmafreefractionsacrossallspeciestested(33-50%),largeVss,highclearanceandintermediateT1/2.  BAY1082439showedstrongp-AKTinhibitionat2and5hourspost-treatmentwhilep-AKTreturnedtolevelscomparabletothevehiclegroupat24hoursinall4tumormodelstested.Interestingly,withoncedailydosing,BAY1082439couldinducetumorregressioninKPL4(PIK3CAmutandHER2+),andtumorstasisinHEC-1B(PTENdel)andinHEC-1A(PIK3CAmut)tumormodels.(source: CancerResearch:April15,2012;Volume72,Issue8,Supplement1doi:10.1158/1538-7445.AM2012-2799.Proceedings:AACR103rdAnnualMeeting2012--Mar31-Apr4,2012;Chicago,IL)  
 
 
 


References

 

苏州蚂蚁淘代理MedKoo在中国的业务。 MedKoo北京代理，MedKoo华东代理，MedKoo华北代理，MedKoo华中代理，MedKoo华南代理,MedKoo全国代理。 MedKoo公司是2009年由Qingqi Chen博士创立。在美国北卡罗来纳州的三角研究园区有运营办公室，其研发和生产车间位于中国。陈博士在加入MedKoo之前，是中山大学药学院（中山大学，中国广州）和中国科学院（北京）“100人计划”的杰出教授。对小分子抗癌药物有浓厚兴趣，发表了100多篇论文，获得20多项。Medkoo是处于先进地位的小分子抗癌试剂，激酶抑制剂和其他相关化学品的优秀供应商。 MedKoo部分产品列表：MedKoo全国代理 406757 10058-F4 530576 10074-G5 600110 10-Deacetylbaccatin III 530429 10-Gingerol 406281 10-Hydroxycamptothecin 341231 10-Hydroxyyohimbine 571387 [11C]-ABP688 526406 11-deoxy-PGF2a 525629 123C4   561223 12-Crown-4 featured 525697 1,3,5,6-Tetrahydroxyxanthone 526087 1,3,5-Trihydroxyxanthone 584120 1,3,7-Trimethyluric acid 527871 1,3-Dicaffeoylquinic acid 530605 1400W HCl