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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Metabolic Enzyme & Protease > BortezomibCAS：179324-69-7
Molecular Formula：C19H25BN4O4
Molecular Weight：384.24
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 179324-69-7 |
| Name | Bortezomib |
| Molecular Formula | C19H25BN4O4 |
| Molecular Weight | 384.24 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 605-854-3 |
| MDL | MFCD09056737 |
| SMILES | OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O |
| InChIKey | GXJABQQUPOEUTA-RDJZCZTQSA-N |
| InChI | InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1 |
| PubChem CID | 387447 |
| Target Point | Proteasome |
| Passage | Metabolic Enzyme&Protease |
| Background | It is a reversible and selective proteasome inhibitor that effectively inhibits the 20S proteasome by targeting threonine residues. Disrupts the cell cycle, induces apoptosis, and inhibits nuclear factor NF-κB. |
| Biological Activity | Bortezomib 是有效的 20S 蛋白酶体 (20S proteasome) 抑制剂，Ki 为 0.6 nM。[1-4] |
| IC50 | Ki: 0.6nM(20S proteasome)[1] |
| In Vitro | 硼替佐米(PS-341)影响控制细胞周期进展的蛋白质。用硼替佐米(100nM)处理PC-3细胞8小时导致细胞在G2-M中积累，G1中细胞数量相应减少。在24和48小时杀死50％的PC-3细胞的硼替佐米剂量分别被确定为100和20nM [1]。硼替佐米是26S蛋白酶体的高选择性，可逆抑制剂。硼替佐米对蛋白酶体的抑制导致JNK的活化，p53，Bid，Bax，p21，p27，caveolin-1和IκBα的稳定化，导致NF-κB的抑制[2]。对于B16F10细胞中的26S蛋白酶体，Bortezomib的IC50为2.46 nM [3]。 |
| In Vivo | 携带Bortezomib(iv，0.3或1.0mg/kg)治疗携带PC-3肿瘤的小鼠。硼替佐米(1.0mg/kg)导致肿瘤生长显著降低~60％。硼替佐米(0.3 mg/kg)可使肿瘤体积减少16％，但未达到显著性[1]。硼替佐米(0.2 mg/kg)在第11天和第15天显著降低戒断阈值，并且与von Frey和丙酮试验中的载体组相比，第11天和第15天的戒断反应数量增加[4]。 |
| Cell Experiment | 在完全培养基中用硼替佐米(0.1nM，1nM，10nM，100nM，1μM，10μM)处理人PC-3前列腺肿瘤细胞24-48小时。使用MTT测定法测量细胞毒性[1]。 |
| Animal Experiment | 小鼠[1]使用雄性裸鼠(18-20g; n = 51)。使用每只小鼠100μL的剂量体积在载体iv中施用硼替佐米(0.3或1.0mg/kg)或以10μL体积直接施用于肿瘤。由于前列腺中相对高水平的硼替佐米，在静脉内给予放射性标记药物后，决定检查这种新化合物在前列腺，PC-3，异种移植肿瘤模型中的作用。当肿瘤变得可触知(> 300mm 3)时，治疗动物。使用雄性裸鼠(18-20g; n = 51)。使用每只小鼠100μL的剂量体积在载体iv中施用硼替佐米(0.3或1.0mg/kg)或以10μL体积直接施用于肿瘤。由于前列腺中相对高水平的硼替佐米，在静脉内给予放射性标记药物后，决定检查这种新化合物在前列腺，PC-3，异种移植肿瘤模型中的作用。当肿瘤变得可触知(> 300mm 3)时，治疗动物。大鼠[4]使用体重200-250g的雄性Sprague-Dawley大鼠。每周两次腹膜内(ip)施用硼替佐米(0.05，0.1或0.2mg/kg)或载体(5％DMSO溶液)，持续2周(在第1，4，8和11天)。硼替佐米的给药方案和剂量基于临床治疗(在第1，4，8和11天为1.3mg/m 2的硼替佐米)确定。 |
| Data Literature Source | [1]. Adams J，et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22. [2]. Boccadoro M，et al. Preclinical evaluation of the proteasome inhibitor bortezomib in cancer therapy. Cancer Cell Int. 2005 Jun 1;5(1):18. [3]. Yerlikaya A，et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9. [4]. Yamamoto S，et al. Behavioral and pharmacological characteristics of bortezomib-induced peripheral neuropathy in rats. J Pharmacol Sci. 2015 Sep;129(1):43-50. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 20mg 50mg |
Examples of using this product（for reference only）
In Vitro:
Cell (Human PCa cell lines (PC3, LNCaP, C4-2, and Du145);3-1000ng/mL bortezomib):
To determine the IC50 concentration of bortezomib (Solarbio), 5×103 cells/well were seeded onto 96-well microtiter plates and were treated with different concentrations (3, 6, 12, 25, 50, 100, 200, 400, 800, and 1000ng/mL) of bortezomib and media supplemented with 5% fetal bovine serum. The CCK-8 assay was then performed to determine the 50% cell proliferation inhibition rate.
Reference：
Fu Z, Lu C, Zhang C, Qiao B. PSMA5 promotes the tumorigenic process of prostate cancer and is related to bortezomib resistance. Anticancer Drugs. 2019 Aug;30(7):e0773. doi: 10.1097/CAD.0000000000000773. PMID: 30807553.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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Fu Z, Lu C, Zhang C, Qiao B. Anticancer Drugs. 2019 Aug;30(7):e0773.
Sorry, there is no more information.
PSMA5 promotes the tumorigenic process of prostate cancer and is related to bortezomib resistance
Click to check >>Author：Fu Z; Lu C; Zhang C; Qiao B
IF：0.0000
Publish_to：Anticancer Drugs
PMID：30807553
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