Birabresib

SKU: orb1301134

Description

Birabresib (MK-8628) is a potent, cell-permeable small molecule inhibitor targeting the BET bromodomain proteins BRD2, BRD3, and BRD4. It has demonstrated antitumor activity in preclinical studies, showing efficacy in both in vitro cellular assays and in vivo models of various cancers, including hematological malignancies and solid tumors.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 202590-98-5
• MW: 491.99
• Purity: 99.93% (May vary between batches)
• Formula: C₂₅H₂₂ClN₅O₂S
• SMILES: CC=1C2=C(N3C([C@H](CC(NC4=CC=C(O)C=C4)=O)N=C2C5=CC=C(Cl)C=C5)=NN=C3C)SC1C
• Target: Epigenetic Reader Domain
• Solubility: DMSO:255 mg/mL (518.3 mM);Ethanol:9.8 mg/mL (19.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.07 mM)

Bioactivity

• Target IC50:
  BRDs:10-19 nM(EC50)
• In Vivo:
  OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively.
• In Vitro:
  Birabresib inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. Birabresib results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines.
• Cell Research:
  Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Epigenetic Reader Domain, EpigeneticReaderDomain, Inhibitor, inhibit, OTX 015, OTX015, OTX-015, OTX015 (MK 8628/Birabresib), MK 8628, MK 8628/Birabresib, MK8628, MK-8628, Birabresib, BRDs

Compound Identifiers

PubChem CID

9936746