Product Name

Mivebresib(ABBV-075)

General description

Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2  nM) and has moderate activity towards CREBBP (Kd = 87 μM 54-fold selectivity vs. BRD4).

Synonym

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

Purity

≥98.5%(HPLC)

CAS Number

1445993-26-9

Formula

C²²H¹⁹F²N³O⁴S

Molecular Weight

459.47

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25°C)

DMSO

≥50mg/mL

Ethanol

Insoluble

Water

Very slightly soluble

l  Biological Information

Biochem/Physiol  Actions

Mivebresib is an inhibitor of one or more as of yet undisclosed bromodomain (BRD)-containing protein(s), with potential antineoplastic activity. Upon administration, mivebresib binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors.

l  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov