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ARV-393

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ARV-393 Basic information

Product Name:
ARV-393
Synonyms:
  • ARV393
  • Acetamide, 2-[[6-[[5-chloro-2-[4-[[trans-3-[4-[2-(2,6-dioxo-3-piperidinyl)-4-fluoro-2,3-dihydro-1-oxo-1H-isoindol-5-yl]-1-piperidinyl]cyclobutyl]oxy]-1-piperidinyl]-4-pyrimidinyl]amino]-1,2-dihydro-1-(1-methylethyl)-2-oxo-3-quinolinyl]oxy]-N-methyl-
  • 2-((6-((5-Chloro-2-(4-(trans-3-(4-(2-(2,6-dioxopiperidin-3-yl)-4-fluoro-1-oxoisoindolin-5-yl)piperidin-1-yl)cyclobutoxy)piperidin-1-yl)pyrimidin-4-yl)amino)-1-isopropyl-2-oxo-1,2-dihydroquinolin-3-yl)oxy)-N-methylacetamide
  • 2-({6-[(5-chloro-2-{4-[(1r,3r)-3-{4-[2-(2,6-dioxopiperidin-3-yl)-4-fluoro-1-oxo-2,3-dihydro-1H-isoindol-5-yl]piperidin-1-yl}cyclobutoxy]piperidin-1-yl}pyrimidin-4-yl)amino]-2-oxo-1-(propan-2-yl)-1,2-dihydroquinolin-3-yl}oxy)-N-methylacetamide
CAS:
2851885-95-3
MF:
C46H53ClFN9O7
MW:
898.42
Mol File:
2851885-95-3.mol
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ARV-393 Chemical Properties

Density 
1.45±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
pka
10.63±0.40(predicted)
form 
Solid
color 
White to off-white
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ARV-393 Usage And Synthesis

Description

ARV-393 is an orally active proteolysis-targeting chimera (PROTAC) that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. It consists of ligand conjugates that target BCL6 and the E3 ligase cereblon, respectively. ARV-393 has demonstrated DC50 and GI50 values of less than 1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). Additionally, it has shown considerable tumor suppressor activity in tumor xenograft models. ARV-393 is currently being studied for its potential to inhibit non-Hodgkin lymphoma.

Biological Functions

ARV-393 is an investigational PROTAC designed to degrade B-cell lymphoma 6 protein (BCL6), a transcriptional repressor and major driver of B-cell lymphomas. The BCL6 protein facilitates B cell tolerance of rapid proliferation and somatic gene recombination via repressing cell cycle checkpoints, terminal differentiation, apoptosis, and the DNA damage response.

target

BCL6

ARV-393 Supplier

Nantong QuanYi Biotechnology Co., Ltd Gold
Tel
0513-66337626 18051384581
Email
sales@chemhifuture.com
Hubei Chuchang Chemical Co., Ltd Gold
Tel
18; 15623560702
Email
Joy.Ren@aliyun.com
Suzhou Haiben Pharmaceutical Co., Ltd Gold
Tel
14760821013 13564957716
Email
1816280386@qq.com
ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266