BiologicalActivity
BETbromodomaininhibitor;blocksrecruitmentofBETtochromatin.InducesapoptosisandG0/G1cellcyclearrestinMLL-fusionleukemiccelllinesinvitro(IC50valuesare15,26,120and192nMforNOMO1,MV4;11,MOLM13andRS4;11celllinesrespectively);reducesBCL2expressioninNOMO1cells.ImprovessurvivalintworodentmodelsofMLL-fusionleukemiainvivo.EnhancesdifferentiationofhumaniPSCintomegakaryocytes.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofI-BET151isreviewedonthechemicalprobeswebsite.
CompoundLibraries
I-BET151dihydrochlorideisalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 488.37 |
| Formula | C23H21N5O3.2HCl |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1883545-47-8 |
| PubChemID | 170320 |
| InChIKey | IQOJZZHRYSSFJM-UHFFFAOYSA-N |
| Smiles | O=C(N3[C@H](C)C4=NC=CC=C4)NC2=C3C1=CC(OC)=C(C5=C(C)ON=C5C)C=C1N=C2.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.54 | 100 | |
| ethanol | 41.54 | 100 | |
| water | 48.84 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight488.37.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.05mL | 10.24mL | 20.48mL |
| 5mM | 0.41mL | 2.05mL | 4.1mL |
| 10mM | 0.2mL | 1.02mL | 2.05mL |
| 50mM | 0.04mL | 0.2mL | 0.41mL |
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