Adipogen/Tozasertib/SYN1092M010/10 mg

MoreInformation
ProductDetails
Synonyms	MK-0457;VX-680
ProductType	Chemical
Properties
Formula	C₂₃H₂₈N₈OS
MW	464.6
CAS	639089-54-6
PurityChemicals	≥95%
Appearance	Solid.
Solubility	SolubleinDMSOorethanol.
Declaration	ManufacturedbySynKinase.
OtherProductData	Target:AuroraA\|KinaseGroup:Other\|Substrate:Serine-Threonine ClickhereforOriginalManufacturerProductDatasheet Ourproductdescriptionmaydifferslightlyfromtheoriginalmanufacturersproductdatasheet.
InChiKey	GCIKSSRWRFVXBI-UHFFFAOYSA-N
ShippingandHandling
Shipping	AMBIENT
ShortTermStorage	+4°C
LongTermStorage	-20°C
Use/Stability	Stableforatleast2yearsafterreceiptwhenstoredat-20°C.
Documents
MSDS	DownloadPDF
ProductSpecificationSheet
Datasheet	DownloadPDF

Inmammals,threeAurorakinases,AuroraA,AuroraB,andAuroraC,areexpressed.AuroraCexpressionismainlyrestrictedtotestis,whereitfunctionsduringmeiosis,whereasAuroraAandBplaykeyfunctionsregulatingmitosis.AuroraAislocalizedtothecentrosomeandspindlepoles,whereitdrivescentrosomematuration,separation,andbipolarspindleassembly.AuroraBisthecentralcomponentofthechromosomalpassengercomplex(CPC)thatalsocontainstheinnercentromereprotein(INCENP),borealin,andsurvivin.Thesenon-enzymaticcomponentsoftheCPCplayakeyroleinregulatingkinaseactivityandlocalization.Over-expressionofAurorakinasescanbeoncogeneicandtheyhavethuslongbeentargetsforcancerthearpy.Tozasertib,orVX-680,isapotentandselectiveinhibitorofAurorakinases,particularlyAuroraAandB.Invitro,VX-680blockscellcycleprogressionandinducesapoptosisinawiderangeofhumantumortypesatlowIC(50)values(i.e.3.38nMforhumanBE-13cells,and14.34nMforNTERAcells).Moreover,VX680,alsohasverypotentKivalues,withinhibitionconstants(Ki)of0.6,18,and46nMforAuroraA,B,andC,respectively.VX-680isalsoeffectiveinvivo,beingusedinaCaki-1xenograftmodel,VX-680demonstrateda75.7%(P<0.001)=""decrease=""in=""caki-1=""xeno-graft=""tumor=""volume=""with=""no=""apparent=""alternation=""in=""animal=""body=""weight,=""peripheral=""blood=""counts,=""or=""other=""biological="">

ProductReferences

VX-680,apotentandselectivesmall-moleculeinhibitoroftheAurorakinases,suppressestumorgrowthinvivo:E.A.Harrington,etal.;Nat.Med.10,262(2004)
Novelseriesofpyrrolotriazineanalogsashighlypotentpan-Aurorakinaseinhibitors:S.Abraham,etal.;Bioorg.Med.Chem.Lett.21,5296(2011)
Developmentofo-chlorophenylsubstitutedpyrimidinesasexceptionallypotentaurorakinaseinhibitors:H.R.Lawrence,etal.;J.Med.Chem.55,7392(2012)

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Adipogen/Tozasertib/SYN1092M010/10 mg