Salinosporamide A (NPI-0052, Marizomib)
(Synonyms: 马里佐米,salinosporamide A, MARIZOMIB, NPI-0052, (-)-Salinosporamide A) 目录号 : GC10486
An orally bioactive proteasome inhibitor
Cas No.:437742-34-2
Sample solution is provided at 25 µL, 10mM.
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Salinosporamide A is a potent inhibitor of 20S proteasome with IC50 value of 1.3 nM [1].
Salinosporamide A was isolated from the crude extract of a Salinospora strain CNB-392. It showed potent anti-tumor activity with an IC50 value of 11 ng/mL in HCT-116 cells. It also exerted a mean GI50 value of less than 10 nM in the NCI’s 60 cell line-panel. Among these cell lines, Salinosporamide A showed the greatest potent efficacies in NCI-H226, SF-539, SK-MEL-28 and MDA-MB-435 cells. Salinosporamide A inhibited the purified 20S proteasome with IC50 value of 1.3 nM. It was about 35-fold more potent than the first discovered specific proteasome inhibitor, omuralide [1].
References:
[1] Feling R H, Buchanan G O, Mincer T J, et al. Salinosporamide A: a highly cytotoxic proteasome inhibitor from a novel microbial source, a marine bacterium of the new genus Salinospora. Angewandte Chemie International Edition, 2003, 42(3): 355-357.
| Cell experiment [1]: | |
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Cell lines |
Human MM-cell lines (MM.1S, INA-6, RPMI-8226, MM.1R,KMS12PE, and U266) |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
24 h; 2nM |
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Applications |
Human MM-cell lines were pretreated with lenalidomide for 24 hours; NPI-0052 was then added for an additional 24 hours, followed by assessment for cell viability using MTT assays. A significant decrease in viability of all cell lines was observed in response to treatment with combined low doses of NPI-0052 and lenalidomide compared with either agent alone(P＜0.05; n=3). These data demonstrate synergistic anti-MM activity of NPI-0052 plus lenalidomide. |
| Animal experiment [2]: | |
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Animal models |
CB-17 SCID-male mice |
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Dosage form |
0.15 mg/kg; i.v. |
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Applications |
MM.1S-tumour bearing mice were injected with NPI-0052(0.15 mg/kg; i.v.) twice a week for 3 weeks, and tumour volume was measured. NPI-0052 treatment significantly decreased tumour growth relative to vehicle-treated control mice (P =0.005). NPI-0052 treatment was not associated with any toxicity, because no differences in body weight and overall appearance were noted. Importantly, the anti-MM activity of NPI-0052 was evident as early as day 5–7, when significant proteasome inhibition was observed in the tumours. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Chauhan D, Singh A V, Ciccarelli B, et al. Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma[J]. Blood, 2010, 115(4): 834-845. [2] Singh A V, Palladino M A, Lloyd G K, et al. Pharmacodynamic and efficacy studies of the novel proteasome inhibitor NPI‐0052 (marizomib) in a human plasmacytoma xenograft murine model[J]. British journal of haematology, 2010, 149(4): 550-559. |
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| Cas No. | 437742-34-2 | SDF | |
| 别名 | 马里佐米,salinosporamide A, MARIZOMIB, NPI-0052, (-)-Salinosporamide A | ||
| 化学名 | (1S,2R,5R)-2-(2-chloroethyl)-5-[(S)-[(1S)-cyclohex-2-en-1-yl]-hydroxymethyl]-1-methyl-7-oxa-4-azabicyclo[3.2.0]heptane-3,6-dione | ||
| Canonical SMILES | CC12C(C(=O)NC1(C(=O)O2)C(C3CCCC=C3)O)CCCl | ||
| 分子式 | C15H20ClNO4 | 分子量 | 313.78 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1869 mL | 15.9347 mL | 31.8695 mL |
| 5 mM | 0.6374 mL | 3.1869 mL | 6.3739 mL |
| 10 mM | 0.3187 mL | 1.5935 mL | 3.1869 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet