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ARV-393

Product Name
ARV-393
CAS No.
2851885-95-3
Chemical Name
ARV-393
Synonyms
ARV393;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;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-methylacetamide;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-
CBNumber
CB614032026
Molecular Formula
C46H53ClFN9O7
Formula Weight
898.42
MOL File
2851885-95-3.mol
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ARV-393 Property

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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Hazard and Precautionary Statements (GHS)

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ARV-393 Chemical Properties,Usage,Production

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.

Uses

ARV-393 is a potent and orally active BCL6 PROTAC degrader. ARV-393 induces ubiquitination of BCL6 and its subsequent degradation by the proteasome. ARV-393 has the potential for the research of advanced non-hodgkin lymphoma[1][2][3].

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.

in vivo

ARV-393 (3, 10, 30 mg/kg; po; once daily for 23 days) shows anticancer activity in xenograft model[3].

Animal Model:Mice (OCI-Ly1 cell line xenograft model)[3]
Dosage:3, 10, 30 mg/kg
Administration:PO; once daily for 23 days (3 mg/kg; twice daily for 23 days)
Result:Ihibited tumor growth and induced BCL6 protein degradation.

target

BCL6

References

[1] Sherman D. Abstract ND05: The discovery of ARV-393, a potent, orally bioavailable BCL6 targeting PROTAC for the treatment of Non-Hodgkin’s Lymphoma[J]. Cancer Research, 2024, 84(7_Supplement): ND05-ND05.
[2] Paolo F. Caimi, et al. Phase 1 Study of ARV-393, a PROTAC BCL6 Degrader, in Advanced Non-Hodgkin Lymphoma. Blood. 2024, 144: 6505.
[3] Paolo Caimi, et al. Abstract PO-010: Trial in Progress: Phase 1 Study of ARV-393, a PROTAC BCL6 Degrader, in Advanced Non-Hodgkin Lymphoma. Blood Cancer Discov. 2024. 5 (3_Supplement): PO-010.

ARV-393 Preparation Products And Raw materials

Raw materials

Preparation Products

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ARV-393 Suppliers

Nantong QuanYi Biotechnology Co., Ltd
Tel
0513-66337626 18051384581
Email
sales@chemhifuture.com
Country
China
ProdList
5975
Advantage
58
Suzhou Haiben Pharmaceutical Co., Ltd
Tel
19353112242
Email
1816280386@qq.com
Country
China
ProdList
8045
Advantage
58
Hubei Chuchang Chemical Co., Ltd
Tel
18 15623560702
Email
info@chuchangbiotech.com
Country
China
ProdList
162
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185;
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4800
Advantage
55
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2961
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9543
Advantage
58
Guangzhou Younan Technology Co., Ltd
Tel
020-82000279 18988941452
Fax
QQ:3283937693
Email
YN_research@163.com
Country
China
ProdList
3000
Advantage
58
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd
Tel
15317229551
Fax
QQ:3607245178
Email
15151849396@163.com
Country
China
ProdList
989
Advantage
58
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View Lastest Price from ARV-393 manufacturers

Shaanxi Dideu New Materials Co. Ltd
Product
ARV-393 2851885-95-3
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
98.0%
Supply Ability
10000KGS
Release date
2025-03-31
Hubei Chuchang Biotech Co., Ltd.
Product
ARV393 2851885-95-3
Price
US $2200.00-3600.00/MG
Min. Order
1MG
Purity
99
Supply Ability
10 G
Release date
2024-06-03

2851885-95-3, ARV-393 Related Search:


  • 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
  • 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-methylacetamide
  • 2851885-95-3