PS-341

  • CAT Number: A000254
  • CAS Number: 179324-69-7
  • Molecular Formula: C₁₉H₂₅BN₄O₄
  • Molecular Weight: 384.24
  • Purity: ≥95%
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Bortezomib is a dipeptide boronic acid analogue with antineoplastic activity. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis. Specifically, the agent inhibits nuclear factor (NF)-kappaB, a protein that is constitutively activated in some cancers, thereby interfering with NF-kappaB-mediated cell survival, tumor growth, and angiogenesis. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy.

Catalog Number A000254
CAS Number 179324-69-7
Molecular Formula

C₁₉H₂₅BN₄O₄

Purity 95%
Target Proteasome
Solubility >19.2mg/mL in DMSO
Storage 3 years -20C powder
InChI InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1
InChIKey GXJABQQUPOEUTA-RDJZCZTQSA-N
SMILES B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
Reference

</br>1: Bockorny M, Chakravarty S, Schulman P, Bockorny B, Bona R. Severe heart failure after bortezomib treatment in a patient with multiple myeloma: a case report and review of the literature. Acta Haematol. 2012;128(4):244-7. doi: 10.1159/000340050. Epub 2012 Sep 4. Review. PubMed PMID: 22964848.</br>2: Broyl A, Jongen JL, Sonneveld P. General aspects and mechanisms of peripheral neuropathy associated with bortezomib in patients with newly diagnosed multiple myeloma. Semin Hematol. 2012 Jul;49(3):249-57. doi: 10.1053/j.seminhematol.2012.04.001. Review. PubMed PMID: 22726548.</br>3: Kapoor P, Ramakrishnan V, Rajkumar SV. Bortezomib combination therapy in multiple myeloma. Semin Hematol. 2012 Jul;49(3):228-42. doi: 10.1053/j.seminhematol.2012.04.010. Review. PubMed PMID: 22726546.</br>4: Sekiguchi Y, Shirane S, Imai H, Sugimoto K, Wakabayashi M, Sawada T, Chigira N, Ichikawa K, Komatsu N, Noguchi M. Response to low-dose bortezomib in plasma cell leukemia patients with malignant pleural effusion and ascites: a case report and a review of the literature. Intern Med. 2012;51(11):1393-8. Epub 2012 Jun 1. Review. PubMed PMID: 22687849.</br>5: Barosi G, Merlini G, Billio A, Boccadoro M, Corradini P, Marchetti M, Massaia M, Tosi P, Palumbo A, Cavo M, Tura S. SIE, SIES, GITMO evidence-based guidelines on novel agents (thalidomide, bortezomib, and lenalidomide) in the treatment of multiple myeloma. Ann Hematol. 2012 Jun;91(6):875-88. doi: 10.1007/s00277-012-1445-y. Epub 2012 Apr 4. Review. PubMed PMID: 22476884.</br>6: Sureshkumar KK, Hussain SM, Marcus RJ, Ko TY, Khan AS, Tom K, Vivas CA, Parris G, Jasnosz KM, Thai NL. Proteasome inhibition with bortezomib: an effective therapy for severe antibody mediated rejection after renal transplantation. Clin Nephrol. 2012 Mar;77(3):246-53. Review. PubMed PMID: 22377258.</br>7: Zangari M, Terpos E, Zhan F, Tricot G. Impact of bortezomib on bone health in myeloma: a review of current evidence. Cancer Treat Rev. 2012 Dec;38(8):968-80. doi: 10.1016/j.ctrv.2011.12.007. Epub 2012 Jan 9. Review. PubMed PMID: 22226939.</br>8: Mujtaba T, Dou QP. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80. Review. PubMed PMID: 22204764.</br>9: Picot J, Cooper K, Bryant J, Clegg AJ. The clinical effectiveness and cost-effectiveness of bortezomib and thalidomide in combination regimens with an alkylating agent and a corticosteroid for the first-line treatment of multiple myeloma: a systematic review and economic evaluation. Health Technol Assess. 2011 Dec;15(41):1-204. doi: 10.3310/hta15410. Review. PubMed PMID: 22146234.</br>10: Delforge M. Bortezomib for previously untreated multiple myeloma. Expert Opin Pharmacother. 2011 Nov;12(16):2553-64. doi: 10.1517/14656566.2011.622266. Epub 2011 Sep 23. Review. PubMed PMID: 21942881.</br>

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