[CAS NO. 1445993-26-9]  Mivebresib (ABBV-075)

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PRODUCTS SPECIFICATIONS [1445993-26-9]

Store
Catalog
SLK-S8400
Brand
Selleck
CAS
1445993-26-9

DESCRIPTION [1445993-26-9]

Overview

MDLMFCD30377200
Molecular Weight459.47
Molecular FormulaC22H19F2N3O4S
SMILESCCS(=O)(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.1764 mL10.8821 mL21.7642 mL
5 mM0.4353 mL2.1764 mL4.3528 mL
10 mM0.2176 mL1.0882 mL2.1764 mL
50 mM0.0435 mL0.2176 mL0.4353 mL

Description

Mivebresib (ABBV-075) is a novel 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). Mivebresib(ABBV-075) efficiently triggers in various tumor cell.

Targets

BRD2 [1]BRD4 [1]BRD-T [1]

In vitro

ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit.