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2851885-95-3

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2851885-95-3 Structure

2851885-95-3 Structure
IdentificationBack Directory
[Name]

ARV393
[CAS]

2851885-95-3
[Synonyms]

ARV393
[Molecular Formula]

C46H53ClFN9O7
[MOL File]

2851885-95-3.mol
[Molecular Weight]

898.42
Chemical PropertiesBack Directory
[density ]

1.45±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
[form ]

Solid
[pka]

10.63±0.40(predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319
[Precautionary statements ]

P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330
Hazard InformationBack Directory
[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.
Spectrum DetailBack Directory
[Spectrum Detail]

ARV-393(2851885-95-3)1HNMR
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