BI-9564

SKU: orb1225830

Description

BI-9564 (BI9564) is a potent, selective, cell-permeable and noncytotoxic BRD9 bromodomain inhibitor with IC50 of 75 nM, Kd of 5,000-fold over BRD4-BD1, BRD4-BD2, and BRD2-BD1; blocks EOL-1 cell proliferation with EC50 of 0.8 uM, and displays antitumor activity in an AML xenograft model.

Key Properties

• CAS Number: 1883429-22-8
• MW: 353.4149
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₃N₃O₃
• SMILES: O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13
• Target: Bromodomain
• Solubility: DMSO: 7.2 mg/mL (Need warming)

Bioactivity

• In Vivo:
  BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for In vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML.
• In Vitro:
  BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, an inhibition > 40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI 9564 | BI9564

Quick Database Links

Gene Symbol

Bromodomain