ARV-771

SKU: orb1301792

Description

ARV-771

Research Area

Epigenetics & Chromatin, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1949837-12-0
• MW: 986.64
• Purity: 99.69%
• Formula: C₄₉H₆₀ClN₉O₇S₂
• SMILES: CC=1C2=C(N3C([C@H](CC(NCCOCCCOCC(N[C@H](C(=O)N4[C@H](C(N[C@@H](C)C5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)C(C)(C)C)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C
• Target: Epigenetic Reader Domain,PROTACs
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.03 mM);DMSO:10 mM

Bioactivity

• Target IC50:
  BRD2(1):34 nM (Kd)|BRD3(1):8.3 nM (Kd)|BRD4(1):9.6 nM (Kd)|BRD4(2):7.6 nM (Kd)|BRD3(2):7.6 nM (Kd)|BRD2(2):4.7 nM (Kd)
• In Vivo:
  METHODS: Nude mice successfully bearing transplanted HepG2 cell tumors were randomly divided into two groups and treated with ARV-771 (20 mg/kg/day, subcutaneous injection) every other day for 25 days. Tumor volume and body weight of mice were measured every 5 days. Immediately after extraction of xenografts from mice, tumor weight was measured by an electronic balance. RESULTS After ARV-771 treatment, tumor volume and tumor weight were significantly reduced. Immunochemical detection results showed that ARV-771 reduced the expression of Ki67 and increased the expression of cleaved Caspase 3 in xenograft tissues.
• In Vitro:
  METHODS: ARV-771 (0.01/0.025/0.05/0.1/0.25/0.5/1/2μM) was used to culture Hep3B, HepG and HCCLM3 cells to observe whether ARV-771 inhibits the growth of these cancer cells. RESULTS ARV-771 had a dose-dependent inhibition on cancer cell viability when the concentration reached 0.25 μM in Hep3B and HepG2 cells and 0.5 μM in HCCLM3 cells.

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

inhibit, EpigeneticReaderDomain, Epigenetic Reader Domain, Inhibitor, ARV 771, ARV771, ARV-771, BET, PROTACs

Compound Identifiers

PubChem CID

126619980