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Background Information:
M-3258 is an orally-bioavailable potent and selective inhibitor of the immunoproteasome subunit LMP7 demonstrating >500-fold selectivity against β1c, β2c, β5c, β1i and β2i. M3258 displayed favorable pharmacokinetics and demonstrated strong LMP7 inhibition and anti-tumor activity in several multiple myeloma xenografts, including models that were refractory to Bortezomib.
Reference:
1. M. Sanderson, et al, First-time disclosure of M3258: A selective inhibitor of the immunoproteasome subunit LMP7 with potential for improved therapeutic utility in multiple myeloma compared to pan-proteasome inhibitors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. Philadelphia (PA): AACR; Cancer Res 2019;79(13 Suppl): Abstract nr DDT02-01.
APIM050047: M-3258
CAS No.: 2285330-15-4.
Molecular Formula: C17H20BNO5.
Molecular Weight: 329.2.
Purity: >99% by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, 1H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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