ARV-771

SKU: orb1301792

Description

ARV-771 is a potent PROTAC-based degrader of BET proteins, exhibiting high affinity for BRD2, BRD3, and BRD4 bromodomains with Kd values in the single-digit nanomolar range. This compound is a valuable chemical probe for investigating BET protein function in cancer research, demonstrating efficacy in both cellular assays and in vivo tumor models.

Research Area

Epigenetics & Chromatin, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1949837-12-0
• MW: 986.64
• Purity: 99.69% (May vary between batches)
• Formula: C₄₉H₆₀ClN₉O₇S₂
• SMILES: O=C([C@H]1N(C([C@H](C(C)(C)C)/N=C(O)/COCCCOCCNC(C[C@H]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2)=O)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
• Target: PROTACs,Epigenetic Reader Domain
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• 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