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

藥理作用：硼替佐米是哺乳動(dòng)物細(xì)胞中26S蛋白酶體糜蛋白酶樣活性的可逆抑制劑。26S蛋白酶體是一種大的蛋白質(zhì)復(fù)合體，可降解泛蛋白。泛蛋白酶體通道在調(diào)節(jié)特異蛋白在細(xì)胞內(nèi)濃度中起到重要作用，以維持細(xì)胞內(nèi)環(huán)境的穩(wěn)定。蛋白水解會(huì)影響細(xì)胞內(nèi)多級(jí)信號(hào)串聯(lián)，這種對(duì)正常的細(xì)胞內(nèi)環(huán)境的破壞會(huì)導(dǎo)致細(xì)胞的死亡。而對(duì)26S蛋白酶體的抑制可防止特異蛋白的水解。體外試驗(yàn)證明硼替佐米對(duì)多種類(lèi)型的癌細(xì)胞具有細(xì)胞毒性。臨床前腫瘤模型體內(nèi)試驗(yàn)證明硼替佐米能夠延遲包括多發(fā)性骨髓瘤在內(nèi)的腫瘤生長(zhǎng)。

本品用于多發(fā)性骨髓瘤患者的**，此患者在使用本品前至少接受過(guò)兩種**，并在*近-次**中病情還在進(jìn)展。

本品外觀為：白色或類(lèi)白色結(jié)晶粉末，易溶于二甲基亞砜，乙醇，難溶于水溶液。

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

LC相關(guān)資料如下:

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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