ARV-771

  Cat. No.:  DC10334   Featured
ARV-771
Chemical Structure
1949837-12-0
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.
Cas No.: 1949837-12-0
Chemical Name:
Synonyms: ARV 771; ARV771
SMILES: CC(C(C(C1=CC=C(Cl)C=C1)=N[C@@H](CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N(C[C@H](O)C2)[C@@H]2C(N[C@H](C3=CC=C(C(SC=N4)=C4C)C=C3)C)=O)=O)=O)=O)C5=NN=C(C)N65)=C6S7)=C7C
Formula: C49H60ClN9O7S2
M.Wt: 986.64
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:
Description: ARV-771 potently degrades BRD2/3/4 in 22Rv1 cells with a DC50 less than 5 nM. c-MYC protein is a downstream effector of BET proteins. Treatment with ARV-771 results in depletion of c-MYC with an IC50 of less than 1 nM. ARV-771 shows strong antiproliferative effect on 22Rv1, VCaP, and LnCaP95 cell lines. ARV-771 treatment has a pronounced effect on cell morphology consistent with apoptosis. FL-AR and AR-V7 mRNA are down-regulated upon treatment with 10 nM ARV-771 in VCaP cells. ARV-771 has an antiandrogenic effect on a number of AR-regulated genes in VCaP cells.Treatment of non castrated male Nu/Nu mice bearing AR-V7+ 22Rv1 tumor xenografts with daily subcutaneous injections of ARV-771 at 10 mg/kg for 3 d results in 37% and 76% down-regulation of BRD4 and c-MYC levels, respectively, in tumor tissue. A marked down-regulation in levels of AR-V7 is observed in the 22Rv1 tumors after ARV-771 treatment.
In Vivo:
In Vitro:
References:
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC10334 ARV-771 ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.