A BRD2

ABBV-075 – 500 µg

Brand:
Cayman
CAS:
1445993-26-9
Storage:
-20
UN-No:
Non-Hazardous - /

ABBV-075 is a potent inhibitor of the bromodomain and extra terminal domain (BET) family of proteins that is selective for the bromodomain-containing proteins (BRD) BRD2, BRD4, and BRDT (Kis = 1-2.2 nM) over BRD3 (Ki = 12.2 nM) and against a panel of 18 BRD proteins.{34796} It inhibits BRD4 recruitment to androgen receptor-occupied gene enhancer sites leading to growth inhibition in androgen receptor-dependent prostate cancer cells.{34795} ABBV-075 halts the cell cycle in the G1 phase and induces apoptosis in prostate cancer cells as well as patient-derived acute myeloid leukemia (AML), non-Hodgkin lymphoma, and multiple myeloma cells.{34794} It is also efficacious in many xenograft mouse models including lung and prostate cancers, AML, and multiple myeloma.{34796,34795,34794} Formulations containing ABBV-075 are in clinical trials for the treatment of advanced hematologic malignancies and solid tumors.  

 

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Description

A BRD2, BRD4, and BRDT inhibitor; selective over BRD3 and against a panel of 18 BRD proteins; inhibits BRD4 recruitment to androgen receptor-occupied gene enhancer sites inhibiting growth in androgen receptor-dependent prostate cancer cells; induces G1 cell cycle arrest and apoptosis in vitro; efficacious in many xenograft mouse models

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

Synonyms:  Mivebresib

Molecular weight: 459.5

CAS: 1445993-26-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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