Bortezomib (PS-341)
Bortezomib (PS-341; CAS 179324-69-7) is a reversible proteasome inhibitor structurally composed as an N-terminally protected dipeptide (Pyz-Phe-boroLeu) containing pyrazinoic acid, phenylalanine, and leucine with boronic acid substitution. It exerts biological activity primarily by inhibiting proteasomal degradation pathways, thereby accumulating pro-apoptotic factors and initiating programmed cell death. Bortezomib inhibits proliferation in cell-based assays, such as human non-small cell lung cancer H460 cells (IC50 = 0.1 µM). It has clinical approval for relapsed multiple myeloma and mantle cell lymphoma, and is widely employed in research to study proteasome-regulated cellular processes and apoptosis signaling pathways.
References:
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 384.24 |
| Cas No. | 179324-69-7 |
| Formula | C19H25BN4O4 |
| Synonyms | Bortezomib,PS-341,LDP-341,MLM341,MG-341,NSC-681239 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥19.21 mg/mL in DMSO |
| Chemical Name | [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid |
| SDF | Download SDF |
| Canonical SMILES | B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Canine malignant melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
72h; IC50=3.5~5.6 nM (nine kinds of cells) |
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Applications |
Bortezomib potently suppressed the growth in 21 drugs, while other compounds had no or minimal effect on cell growth. We thus focused on bortezomib and examined its growth inhibitory properties against nine canine malignant melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML). Bortezomib inhibited the growth of all cell lines with calculated IC50 values of 3.5~5.6 nM. |
| Animal experiment [1]: | |
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Animal models |
Nude athymic mice |
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Dosage form |
0.8 mg/kg; intravenous injection |
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Applications |
The in vivo growth inhibitory activity of bortezomib against CMM-1 cells was evaluated using a xenograft mouse model. Bortezomib significantly suppressed the growth of tumours after Day 4 of treatment (P < 0.01, control vs. bortezomib). Tumours from the bortezomib-treated mice showed a significant decrease in mitotic index compared to controls (P |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Ito K, Kobayashi M, Kuroki S, et al. The proteasome inhibitor bortezomib inhibits the growth of canine malignant melanoma cells in vitro and in vivo[J]. The Veterinary Journal, 2013, 198(3): 577-582. |
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| Description | Bortezomib (PS-341) is a potent inhibitor of 20S proteasome with Ki of 0.6 nM. | |||||
| Targets | 20S proteasome | |||||
| IC50 | 0.6 nM (Ki) | |||||
Quality Control & MSDS
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