ARV-393
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
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
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.
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 Supplier
- Tel
- 0513-66337626 18051384581
- sales@chemhifuture.com
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- 18 15623560702
- info@chuchangbiotech.com
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- 19353112242
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- 18149758185
- sales-cpd@caerulumpharma.com
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- 021-52996696，15000506266 15000506266