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B-1408 Bortezomib, Free Base, 99%

[Velcade] [MG-341] [PS-341]

M.W. 384.24

C19H25BN4O4

[179324-69-7]

M.I. 14:  1351

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 200 mg/mL; soluble in ethanol at 200 mg/mL; very poorly soluble 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.  Disposal:  A

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• Potent (Ki, 0.6 nM), specific and reversible proteasome inhibitor; no significant inhibitory activity against other enzymes or receptors.  Bouchard, PR., et al.  "Nonclinical Discovery and Development of Bortezomib (PS-341, Velcade®), a Proteasome Inhibitor for the Treatment of Cancer."  55th Annual Meeting of the American College of Veterinary Pathologists (ACVP) & 39th Annual Meeting of the American Society of Clinical Pathology (ASVCP), ACVP and ASVCP (Eds.) (2004).

• In a study with the National Cancer Institute's panel of 60 human cell lines, bortezomib showed a mean IC50 of 7 nM as tested by SRB analysis.  Adams, J., et al.  "Proteasome inhibitors: a novel class of potent and effective antitumor agents."  Cancer Res. 59:  2615-2622 (1999).

• Bortezomib is active in preclinical models of human prostate cancer, while its effects on apoptosis versus angiogenesis are cell type dependent.  Bortezomib caused comparable growth suppression in LNCaP-Pro5 and PC3M-Pro4 cells with an IC90 of 10 nM.  Williams, S., et al.  "Differential effects of the proteasome inhibitor bortezomib on apoptosis and angiogenesis in human prostate tumor xenografts."  Mol. Cancer Ther. 2:  835-843 (2003).

• Bortezomib inhibits cell proliferation of H460 cells (Human non-small cell lung cancer cell lines) with an IC50 of 0.1 µM.  Ling, Y., et al.  "Mechanisms of Proteasome Inhibitor PS-341-induced G2-M-Phase Arrest and Apoptosis in Human Non-Small Cell Lung Cancer Cell Lines." Clin. Cancer Res. 9:  1145-1154 (2003).

• Bortezomib is the active ingredient in the drug sold under the trade name Velcade®.  This drug has been approved in at least one country to treat multiple myeloma.  NOTE:  The bortezomib sold by LC Laboratories is NOT Velcade®, and is NOT for human use.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.