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Bpsbioscience/SGI1776 free base/276512/10 mg
MW:405.4Da
CASRegistry#:1025065-69-3
Formula:C20H22F3N5O
Target:Pim1
Background:
Accordingtopreliminaryresultsfromstudiestreatingprostatecancercells,SGI-1776dose-dependentlyreducesphosphorylationofknownPimkinasesubstratesinvolvedincellcycleprogressionandapotosis(p21Cip1/WAF1andBad),compromisesoverallcellviabilitybyinducingG1cellcyclearrestandtriggeringapoptosis,andreducescellviabilityinamultidrugresistance1(MDR1)proteinbasedtaxane-refractoryprostatecancercellline.
Description:
SGI-1776isapotentATP-competitiveinhibitoroftheserine/threoninefamilyofPimkinase,anenzymeregulatingcellsurvival.Throughextensivebiomedicalcharacterization,SGI-1776exhibitsspecificitytothethreeisoformsofthePimfamily,includingPim-1,Pim-2,andPim-3.TreatmentwithSGI-1776inducesapoptosisinCLLprimarycellline.
Synonym(s):
N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
Purity:

≥98%byHPLC

BiologicalActivity:
SGI-1776inhibitsPim1,Pim2,Pim3,andFLT3withIC50valuesof7nM,363nM,69nM,and44nMrespectively.
Solubility:
SolubleinDMSO
Storage/Stability:

Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.

Reference(s):
1.Mumenthaler,SM.,etal.MolCancerTher.2009;8(10):2882-2893.
2.LisaS.Chen,LSetal.Blood.2009;114(19):4150-4157.
ScientificCategory:
KinaseInhibitors
ProductType:
Inhibitor
Datashownislot-specific.Contactusforspecificinformationonotherlots.

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