Bortezomib;硼替佐米;保特佐米; Velcade;MG-341;PS-341;

硼替佐米Bortezomib

中文名：保特佐米, 硼替佐米

英文名：Bortezomib

[(1R)-3-甲基-1-[[(2S)-1-氧-3-苯基-2-[(吡嗪甲酰)氨基]丙基]氨基]丁基]-硼酸

[(1r)-3-methyl-1-[[(2s)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]-boronic acid

CAS No.:179324-69-7

Molecular Formula: C₁₉H₂₅BN₄O₄

Molecular Weight: 384.24

药理作用：硼替佐米是哺乳动物细胞中26S蛋白酶体糜蛋白酶样活性的可逆抑制剂。26S蛋白酶体是一种大的蛋白质复合体，可降解泛蛋白。泛蛋白酶体通道在调节特异蛋白在细胞内浓度中起到重要作用，以维持细胞内环境的稳定。蛋白水解会影响细胞内多级信号串联，这种对正常的细胞内环境的破坏会导致细胞的死亡。而对26S蛋白酶体的抑制可防止特异蛋白的水解。体外试验证明硼替佐米对多种类型的癌细胞具有细胞毒性。临床前肿瘤模型体内试验证明硼替佐米能够延迟包括多发性骨髓瘤在内的肿瘤生长。

本品用于多发性骨髓瘤患者的**，此患者在使用本品前至少接受过两种**，并在*近-次**中病情还在进展。

本品外观为：白色或类白色结晶粉末，易溶于二甲基亚砜，乙醇，难溶于水溶液。

Very soluble in DMSO or ethanol, up to about 200 mg/mL; poorly soluble in aqueous solution

LC相关资料如下:

B-1408 Bortezomib, 99%  

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 200 mg/mL; soluble in ethanol at 200 mg/mL; soluble in water at 3 mg/mL; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

View the MSDS for this product

·          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 is approved to treat multiple myeloma.

·          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) Section 68B of the Patents Act of 1953 in New Zealand; (vi) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (vii) 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.

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