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- 保存条件：
见说明书
- 保质期：
＞1年
- 英文名：
Bortezomib Free Base
- 库存：
期货2-3周
- 供应商：
上海经科化学科技有限公司
- CAS号：
179324-69-7
- 规格：
5mg
供应商：上海经科化学科技有限公司
服务热线：400-0199-638
QQ:472482400(上海经科）
微信号：shjkchem
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本试剂(Bortezomib)
仅供科研实验使用,不得用于其他用途！
货 号：B-1408
名 称：Bortezomib
别 名：Bortezomib Free Base
C A S ：179324-69-7
分子量：384.24
分子式：C19H25BN4O4
纯 度：HPLC/TLC:>99%
说 明：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.
文 献：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).
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文献和实验Proteasome Inhibitors in Cancer Therapy
bortezomib (VELCADE�, formerly known as PS-341), has recently been approved in the United States for treatment of patients with multiple myeloma who have received at least two prior therapies, and have demonstrated disease progression on their last therapy
远多于女性患者，黑人患骨髓瘤的机率是白人的 2 倍以上。导致骨髓瘤发生的因素较多，例如遗传、辐射或化学物接触等。目前市场上已有 bortezomib，PEGylated liposomal doxorubicin[3]等药物用于治疗多发性骨髓瘤，且免疫调节药物（IMiD）来那度胺联合蛋白酶体抑制剂硼替佐米和地塞米松可有效治疗骨髓瘤。硼替佐米和来那度胺可杀伤骨髓瘤细胞并克服其对传统治疗的耐药，但多发性骨髓瘤仍然不可治愈。事实上，几乎所有的多发性骨髓瘤患者在接受治疗后，最终还是会产生耐药性，从而导致
王红阳院士等 Science 子刊报道老药新用的精准治疗机制，为 PTEN 突变肿瘤治疗带来新思路
）, 并将其用于药物筛选和分子谱分析，以寻找个性化的治疗方法和治疗机制。通过使用69种经过FDA批准的抗癌药库，对96孔板中培养的10个PDCs进行药物筛选测定，作者发现蛋白酶体抑制剂硼替佐米（bortezomib，多发性骨髓瘤治疗药物）对PDCs具有强大的细胞毒性作用。通过对胆管癌细胞系验证发现，不同细胞系对蛋白酶抑制剂的敏感性有所不同。 图片来源：Science Translational Medicine为了探究导致敏感性差异的机制，作者对两种代表性细胞系HCCC-9810（敏感）和RBE（不敏感）的进
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