LMP7-IN-1 manufacturers
- M3258
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2026-07-14
- CAS:2285330-15-4
- Purity: 99.91%
- Supply Ability: 10g
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| | LMP7-IN-1 Basic information |
| Product Name: | LMP7-IN-1 | | Synonyms: | LMP7-IN-1;M-3258;M3258，LMP7-IN-1;M3258,M-3258;Boronic acid, B-[(1R)-2-(3-benzofuranyl)-1-[[(1S,2R,4R)-7-oxabicyclo[2.2.1]hept-2-ylcarbonyl]amino]ethyl]- | | CAS: | 2285330-15-4 | | MF: | C17H20BNO5 | | MW: | 329.16 | | EINECS: | | | Product Categories: | | | Mol File: | 2285330-15-4.mol |  |
| | LMP7-IN-1 Chemical Properties |
| density | 1.328±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 250 mg/mL (759.51 mM) | | form | Solid | | pka | 9.56±0.43(Predicted) | | color | White to off-white |
| | LMP7-IN-1 Usage And Synthesis |
| Uses | M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells[1][2]. | | in vivo | M3258 (1 mg/kg; 10 mg/kg) shows superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib[2]. | Animal Model: | Female H2d Rag2 mice or female CB-17 SCID mice (U266B1 subcutaneous xenograft model; MM.1S subcutaneous xenograft model)[2] | | Dosage: | 1 mg/kg in U266B1 subcutaneous xenograft model; 10 mg/kg in MM.1S subcutaneous xenograft model | | Administration: | P.o.; either once daily, every 2 days or twice weekly (days 1 and 4) | | Result: | Displayed significant and strong antitumor efficacy. |
| | References | [1] Klein M, et al. Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) [published online ahead of print, 2021 Jul 6]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00604. DOI:10.1021/acs.jmedchem.1c00604
[2] Sanderson MP, et al. M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models [published online ahead of print, 2021 May 27]. Mol Cancer Ther. 2021;10.1158/1535-7163.MCT-21-0005. DOI:10.1158/1535-7163.MCT-21-0005 |
| | LMP7-IN-1 Preparation Products And Raw materials |
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