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Mivebresib

Chemical Structure : Mivebresib

CAS No.: 1445993-26-9

Mivebresib (ABBV-075;ABBV075)

Catalog No.: PC-42029Not For Human Use, Lab Use Only.

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.

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Biological Activity

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.
Mivebresib (ABBV-075) displays 54-fold selectivity over EP300, has potential weak activity against SMARCA4 (70% inhibition at 1 uM), Kd >1 uM for 18 other bromodomains.
Mivebresib (ABBV-075) exhibits inhibition of c-Myc expression and displacing BRD4 from the Myc promoter.
Mivebresib (ABBV-075) 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.

Physicochemical Properties

M.Wt 459.4658
Formula C22H19F2N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 37 mg/mL

Chemical Name/SMILES

Ethanesulfonamide, N-[4-(2,4-difluorophenoxy)-3-(6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]-

References

1. McDaniel KF, et al. J Med Chem. 2017 Oct 26;60(20):8369-8384.

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