Mivebresib
Mivebresib (ABBV-075) is a potent and orally available BET bromodomain inhibitor with Ki of 1.0, 12.2, 1.5, and 2.2 nM for BRD2, BRD3, BRD4 and BRDT, respectively; displays 54-fold selectivity over EP300, has potential weak activity against SMARCA4 (70% inhibition at 1 uM), Kd >1 uM for 18 other bromodomains; exhibits inhibition of c-Myc expression and displacing BRD4 from the Myc promoter; dose-dependently inhibits IL-6 concentration in a murine model of LPS-induced endotoxic shock, shows vivo antitumor efficacy in a Kasumi-1 AML mouse xenograft model.Breast Cancer Phase 1 Clinical (In Vitro) :Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.
Product Specifications
CAS Number
1445993-26-9
Product Name Alternative
ABBV-075 | ABBV075
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 37 mg/mL
Smiles
CCS (=O) (NC1=CC=C (OC2=CC=C (F) C=C2F) C (C3=CN (C) C (C4=C3C=CN4) =O) =C1) =O
Molecular Formula
C22H19F2N3O4S
Molecular Weight
459.4658
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Ethanesulfonamide, N-[4- (2,4-difluorophenoxy) -3- (6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl) phenyl]-
Available Sizes
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