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Bortezomib (CAS 179324-69-7)

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Alternate Names:
Bortezomib also known as Velcade; Radiciol; LDP-341
Application:
Bortezomib is a selective and robust 26S proteasome inhibitor and is a boronic acid dipeptide derivative
CAS Number:
179324-69-7
Purity:
≥98%
Molecular Weight:
384.24
Molecular Formula:
C19H25BN4O4
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Bortezomib is a selective and robust 26S proteasome inhibitor, that is a boronic acid dipeptide derivative. Human pancreatic cancer cell studies demonstrate Bortezomib to inhibit the PKR-like endoplasmic reticulum (ER) kinase and enhance ER stress, leading to apoptosis. Studies suggest that Bortezomib affects the gene expression of WT1, and blocks the function of human plasmacytoid DCs through the inhibition of intracellular trafficking of Toll-like receptors and modification of the ER homeostasis. Additionally, Bortezomib has been reported to inhibit necrosis and cell proliferation, and downregulate metastatic gene expression. Bortezomib is an inhibitor of 20S Proteasome.


Bortezomib (CAS 179324-69-7) References

  1. Proteasome inhibition measurements: clinical application.  |  Lightcap, ES., et al. 2000. Clin Chem. 46: 673-83. PMID: 10794750
  2. Development of the proteasome inhibitor PS-341.  |  Adams, J. 2002. Oncologist. 7: 9-16. PMID: 11854543
  3. Mechanisms of proteasome inhibitor PS-341-induced G(2)-M-phase arrest and apoptosis in human non-small cell lung cancer cell lines.  |  Ling, YH., et al. 2003. Clin Cancer Res. 9: 1145-54. PMID: 12631620
  4. Bortezomib inhibits PKR-like endoplasmic reticulum (ER) kinase and induces apoptosis via ER stress in human pancreatic cancer cells.  |  Nawrocki, ST., et al. 2005. Cancer Res. 65: 11510-9. PMID: 16357160
  5. A proteasome inhibitor, bortezomib, inhibits breast cancer growth and reduces osteolysis by downregulating metastatic genes.  |  Jones, MD., et al. 2010. Clin Cancer Res. 16: 4978-89. PMID: 20843837
  6. Bortezomib suppresses function and survival of plasmacytoid dendritic cells by targeting intracellular trafficking of Toll-like receptors and endoplasmic reticulum homeostasis.  |  Hirai, M., et al. 2011. Blood. 117: 500-9. PMID: 20956804
  7. Erythroid response and decrease of WT1 expression after proteasome inhibition by bortezomib in myelodysplastic syndromes.  |  Alimena, G., et al. 2011. Leuk Res. 35: 504-7. PMID: 20971509
  8. Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system.  |  Dou, QP. and Zonder, JA. 2014. Curr Cancer Drug Targets. 14: 517-36. PMID: 25092212
  9. NEK2 induces autophagy-mediated bortezomib resistance by stabilizing Beclin-1 in multiple myeloma.  |  Xia, J., et al. 2020. Mol Oncol. 14: 763-778. PMID: 31955515
  10. Bortezomib alleviates myocardial ischemia reperfusion injury via enhancing of Nrf2/HO-1 signaling pathway.  |  Liu, C., et al. 2021. Biochem Biophys Res Commun. 556: 207-214. PMID: 33848935
  11. Bortezomib-Induced Ovarian Toxicity in Mice.  |  Mutluay, D., et al. 2022. Toxicol Pathol. 50: 381-389. PMID: 35352576
  12. Bortezomib-resistant multiple myeloma patient-derived xenograft is sensitive to anti-CD47 therapy.  |  Yue, Y., et al. 2022. Leuk Res. 122: 106949. PMID: 36113267
  13. Bortezomib-induced neurotoxicity in human neurons is the consequence of nicotinamide adenine dinucleotide depletion.  |  Snavely, AR., et al. 2022. Dis Model Mech. 15: PMID: 36398590

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Bortezomib, 2.5 mg

sc-217785
2.5 mg
$132.00

Bortezomib, 25 mg

sc-217785A
25 mg
$1064.00

Refractive index given as predicted for bortezomib. Can you please explain what was the method/instrument you have been employed for the estimation of this predicted value.

Asked by: Samp
Thank you for your question. The refractive index listed on our website was a predicted value taken from ChemSpider.
Answered by: Technical Support
Date published: 2019-02-01

Do you have safety information on working with this drug in solution? I want to feed small amounts of it to fruit flies (dissolve the drug in dmso and mix into standard fly food) and wonder about exposure limits of the dissolved drug for researchers.

Asked by: Drosophilist
Thank you for your question. Please refer to the SDS Section 11 for toxicological information for this chemical, Bortezomib: sc-217785. http://datasheets.scbt.com/sds/aghs/en/sc-217785.pdf
Answered by: Technical Support
Date published: 2017-05-17

Is this soluble in aqueous buffers?

Asked by: SCchem16
Thank you for your question. This chemical, Bortezomib (CAS 179324-69-7), is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, bortezomib should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. Bortezomib has a solubility of approximately 0.1 mg/ml in a 1:5 solution of DMSO:PBS (pH 7.2) using this method.
Answered by: Chemical Support 2
Date published: 2017-02-24

Guten Tag. Liefern Sie Ihre Medikamenten Weltweit aus? Z.b. nach Taschkent/Usbekistan? MfG. A.Sudorgin

Asked by: sascha1962
Sehr geehrte,r A. Sudorgin, herzlichen Dank für Ihre Anfrage. Santa Cruz Biotechnology, Inc. bietet ausschließlich in-vitro Forschungsreagenzien für die Grundlagenforschung an. Forschungsreagenzien liefern wir gerne an institutionelle Kunden in Taschkent/Usbekistan. Thank you very much for your question. All Santa Cruz Biotechnology, Inc. products are sold for in-vitro research or laboratory use only (RUO) and are not to be administered to humans or used for medical diagnostics. Researchers located in Tashkent / Republic of Uzbekistan might want to contact our European Support office <europe@scbt.com> regarding product inquiries.
Answered by: Technical Support Europe
Date published: 2017-02-22

Hi. How would you dissolve and inject bortezomib in mice? Do you have a specific protocol for this?

Asked by: Pierre
Thank you for your question. This chemical, bortezomib, is soluble in chloroform, DMSO (200 mg/ml), ethanol (200 mg/ml), and methanol. Partly miscible in water.Maximum solubility in plain water is estimated to be about 5-10 µM. Buffers, serum, or other additives may increase or decrease the aqueous solubility. Unfortunately we are not able to provide injection information. Our compounds are not pharmaceutical grade and not manufactured under GMP guidelines. Please consult your principal investigator and your animal care and use committee (ACUC) regarding the use of our compounds. Please contact Technical Service by phone, (800)-457-3801 option 2, email <scbt@scbt.com>, or by live chat directly on our website, www.scbt.com if you have any further questions.
Answered by: Tech Service
Date published: 2017-01-12

What is the stability of the product after solubilized?

Asked by: two2igm05
Thank you for your question. Bortezomib, sc-217785, is stable for 2 years at -20°C as a powder, for 2 weeks at 4°C in DMSO, and for 6 months at -80°C in DMSO.
Answered by: TechService7
Date published: 2017-01-04
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Rated 5 out of 5 by from Great reagent! works well!we bought this product fews weeks ago and it has been working well for us. The effect expected was seen with it! Thank you! Marina
Date published: 2017-11-13
Rated 5 out of 5 by from Alimena et alAlimena et al. (PubMed ID 20971509) found that Bortezomib, a 26S proteasome inhibitor, decreased WT1 gene expression in patients with myelodysplastic syndrome. -SCBT Publication Review
Date published: 2015-01-13
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Bortezomib is rated 5.0 out of 5 by 2.
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