MedKoo Biosciences/AT13148/205884/25mg

AT13148isanoveloralmulti-AGCkinaseinhibitorwithpotentpharmacodynamicandantitumoractivity,whichshowsadistinctmechanismofactionfromotherAKTinhibitors.AT13148iscurrentlybeingdevelopedbyAstexPharmaceuticals.AT131148wasidentifiedutilizinghigh-throughputX-raycrystallographyandfragment-basedleaddiscoverytechniques.AT13148causedsubstantialblockadeofAKT,p70S6K,PKA,ROCKandSGKsubstratephosphorylationandinductionofapoptosisinbothaconcentrationandtime-dependentmannerincancercellswithclinicallyrelevantgeneticdefectsbothinvitroandinvivo.

MedKooCat#:205884
Name:AT13148
CAS#:1056901-62-2
ChemicalFormula:C17H16ClN3O
ExactMass:313.09819
MolecularWeight:313.78
ElementalAnalysis:C,65.07;H,5.14;Cl,11.30;N,13.39;O,5.10

Synonym:AT-13148;AT13148;AT13148.

IUPAC/ChemicalName:(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol

InChiKey:IIRWNGPLJQXWFJ-KRWDZBQOSA-N

InChiCode:InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22,11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10,22H,11,19H2,(H,20,21)/t17-/m0/s1

SMILESCode:ClC1=CC=C([C@](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1

TechnicalData

Appearance:

whitesolidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:

ViewcurrentbatchofCoA

QCData:

ViewNMR,ViewHPLC,ViewMS

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

AT13148isanorallyactivesmallmoleculeinhibitorofPKB/Aktandp70S6kinase,keyenzymesinthePI3K/PKB/mTORtumorcellsurvivalpathway.AT13148hasthepotentialtobeaveryeffectiveinhibitorofAKTdependenttumors.InSeptember2008AstexannouncedapartnershipwithCancerResearchUKandCRTtotakeAT13148intodevelopmentunderthecharity'sClinicalDevelopmentPartnerships(CDP)program.Underthetermsofthisagreement,CancerResearchUK'sDrugDevelopmentOfficehascarriedoutfurtherdevelopmentworkontheagent,someofwhichisdoneincollaborationwiththeICR.CRUKplanstocommencephase1clinicaltrialsofAT13148attheRoyalMarsdenHospitalintheUKduring2012. (source:http://astx.com/pipeline/products/clinical).

References

1:YapTA,WaltonMI,GrimshawKM,TePoeleRH,EvePD,ValentiMR,deHavenBrandonAK,MartinsV,ZetterlundA,HeatonSP,HeinzmannK,JonesPS,FeltellRE,ReuleM,WoodheadSJ,DaviesTG,LyonsJF,RaynaudFI,EcclesSA,WorkmanP, ThompsonNT,GarrettMD.AT13148isanovel,oralmulti-AGCkinaseinhibitorwithpotentpharmacodynamicandantitumoractivity.ClinCancerRes.2012Jul15;18(14):3912-23.doi:10.1158/1078-0432.CCR-11-3313.Epub2012Jul10.PubMedPMID:22781553.

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MedKoo Biosciences/AT13148/205884/25mg

TechnicalData

AdditionalInformation

References