A BD2 bromodomain inhibitor (Kis = 4.6

ABBV-744 – 5 mg

Brand:
Cayman
CAS:
2138861-99-9
Storage:
-20
UN-No:
Non-Hazardous - /

ABBV-744 is an inhibitor of the bromodomain and extra-terminal domain (BET) family protein bromodomain 2 (BD2; Kis = 4.6, 4.9, 1.6, and 1 nM for BRD2, -3, -4, and -T, respectively).{58046} It is selective for BD2 over BD1 bromodomains in a time-resolved FRET (TR-FRET) assay (Kis = 1,162, 3,140, 521, and 917 nM for BRD2, -3, -4, and -T, respectively). ABBV-744 inhibits proliferation of SKM-1 leukemia cells (IC50 = 6.7 nM). It induces cell cycle arrest at the G1 phase in LNCaP prostate cancer cells.{58047} ABBV-744 (18.8 mg/kg) reduces tumor volume in a SKM-1 mouse xenograft model.{58046} It also reduces tumor growth in LNCaP and MDA PCa 2b mouse xenograft models when administered at doses of 1 and 4.7 mg/kg.{58047}  

 

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SKU: 30470 - 5 mg Category:

Description

A BD2 bromodomain inhibitor (Kis = 4.6, 4.9, 1.6, and 1 nM for BRD2, -3, -4, and -T, respectively); selective for BD2 over BD1 bromodomains in a TR-FRET assay (Kis = 1,162, 3,140, 521, and 917 nM for BRD2, -3, -4, and -T, respectively); inhibits proliferation of SKM-1 leukemia cells (IC50 = 6.7 nM); induces cell cycle arrest at the G1 phase in LNCaP cells; reduces tumor volume in a SKM-1 mouse xenograft model at 18.8 mg/kg; reduces tumor growth in LNCaP and MDA PCa 2b mouse xenograft models at 1 and 4.7 mg/kg

Formal name: N-ethyl-4-[2-(4-fluoro-2,6-dimethylphenoxy)-5-(1-hydroxy-1-methylethyl)phenyl]-6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide

Synonyms: 

Molecular weight: 491.6

CAS: 2138861-99-9

Purity: ≥98%

Formulation: A crystalline solid

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