2089390-09-8
Chemical Structure
Zavabresib
Synonym(s): OPN-2853; PLX2853; BET-IN-16
- CAS No.: 2089390-09-8
- Formula:C31H25N5O3
- Molecular Weight:515.56
InChIKey: LLUTURRCWNCHPC-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(C2=CN(C(C3=NC=CC=C3)(C)C4=NC=CC=C4)C5=C2N=CC(C6=C(C)ON=C6C)=C5)C=C1)O
Biological Activity: Zavabresib (OPN-2853; PLX2853; BET-IN-16) is an orally active inhibitor of the BET family of proteins. Zavabresib blocks bromodomain-mediated interactions, reduces BRD4 enrichment at the regulatory regions of transcription factors in T cells, exerts tumor growth inhibitory effects, and enhances the efficacy of immunotherapy. Zavabresib is applicable to research on chronic lymphocytic leukemia, castration-resistant prostate cancer, diffuse large B-cell lymphoma, colon adenocarcinoma, and myelofibrosis[1][2][3][4][5].
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Zavabresib | 99.60% | Zavabresib (OPN-2853; PLX2853; BET-IN-16) is an orally active inhibitor of the BET family of proteins. Zavabresib blocks bromodomain-mediated interactions, reduces BRD4 enrichment at the regulatory regions of transcription factors in T cells, exerts tumor growth inhibitory effects, and enhances the efficacy of immunotherapy. Zavabresib is applicable to research on chronic lymphocytic leukemia, castration-resistant prostate cancer, diffuse large B-cell lymphoma, colon adenocarcinoma, and myelofibrosis. | ||||||||||||||||||||
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References
- [1]. Smith AL, et al. BET inhibition reforms the immune microenvironment and alleviates T cell dysfunction in chronic lymphocytic leukemia. JCI insight. 2024 May 22;9(10):e177054.
- [2]. Duska LR, et al. Phase IIa Study of PLX2853 in Gynecologic Cancers With Known ARID1A Mutation and Phase Ib/IIa Study of PLX2853/Carboplatin in Platinum-Resistant Epithelial Ovarian Cancer. JCO precision oncology. 2023 Sep;7:e2300235.
- [3]. Wang S, et al. Method for administration of an anti cancer agent. WO2021175824A1. WIPO‑PCT. 2021‑09‑10.
- [4]. Powell B, et al. Combinational drug anticancer therapies. WO2022040512A1. WIPO‑PCT. 2022‑02‑24.
- [5]. Gordon MS, et al. BET inhibitor OPN-2853 in advanced solid tumors and lymphoma: results from the phase 1b PLX124-01 trial. Cancer Chemother Pharmacol. 2026 Mar 6;96(1):20.
