规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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体外研究 (In Vitro) |
PlinabuLin (NPI-2358) 是一种有效的抗肿瘤药物,可在多重耐药 (MDR) 肿瘤细胞系中快速诱导微管蛋白解聚和单层通透性。在 HUVEC 中,DU 145 细胞的 IC50 值为 18 nM,PC-3 细胞为 13 nM,MDA-MB-231 细胞为 14 nM,NCI-H292 细胞为 18 nM,Jurkat 白血病细胞为 11 nM。纳米[1]。
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体内研究 (In Vivo) |
当给予普那布林(0 mg/kg–15 mg/kg;腹膜内注射)时,雌性 CDF1 和 C3H/He 小鼠的肿瘤灌注以剂量和时间依赖性方式减少。普那布林的抗癌作用对 KHT 肉瘤比对 C3H 肿瘤更敏感,并且两种模型均表现出增强的放射反应 [3]。
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细胞实验 |
细胞活力测定[1]
细胞类型: HUVEC 细胞 测试浓度: 2 nM、10 nM、20 nM 和 200 nM 孵育时间:30 分钟 实验结果:低浓度(2 nM、10 nM)快速诱导 HUVEC 中微管蛋白解聚。 |
动物实验 |
Animal/Disease Models: Female CDF1 mice (10-14weeks old) with C3H mammary carcinoma; Female C3H/HeJ mice with KHT sarcoma cells (8-weeks-old)[3]
Doses: 0 mg/kg, 1.5 mg/kg , 2.5 mg/kg, 5 mg/kg, 7.5 mg/kg, 10 mg/kg, 12.5 mg/kg, 15 mg/kg; 0.02 mL/g mouse body weight in CDF1 mice and 0.01 mL/g body weight for C3H /HeJ mice Route of Administration: intraperitoneal (ip)injection; 0 huor, 1 huor, 3 hrs (hours), 6 huors, 24 huors Experimental Results: Induced a time- and dose-dependent decrease in tumour perfusion. The KHT sarcoma was more sensitive than the C3H tumour to the anti -tumor, while radiation response was enhanced in both models. |
参考文献 |
[1]. Nicholson B et al. NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Anticancer Drugs. 2006 Jan;17(1):25-31.
[2]. Monica M. Mita et al. Phase 1 First-in-Human Trial of the Vascular Disrupting Agent Plinabulin (NPI-2358) in Patients with Solid Tumors or Lymphomas Clin Cancer Res. 2010 Dec 1;16(23):5892-9. [3]. Bertelsen LB, et al. Vascular effects of plinabulin (NPI-2358) and the influence on tumour response when given alone or combined with radiation. Int J Radiat Biol. 2011 Nov;87(11):1126-34. |
分子式 |
C19H20N4O2
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分子量 |
336.39
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CAS号 |
714272-27-2
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相关CAS号 |
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SMILES |
O=C(/C(NC/1=O)=C\C2=CC=CC=C2)NC1=C\C3=C(C(C)(C)C)NC=N3
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化学名 |
(3E,6E)-3-benzylidene-6-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)piperazine-2,5-dione
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别名 |
NPI-2358; Plinabulin; NPI2358; NPI 2358;
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9727 mL | 14.8637 mL | 29.7274 mL | |
5 mM | 0.5945 mL | 2.9727 mL | 5.9455 mL | |
10 mM | 0.2973 mL | 1.4864 mL | 2.9727 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05599789 | Recruiting | Drug: Pembrolizumab in Combination with Plinabulin and Docetaxel |
Non Small Cell Lung Cancer Metastatic |
Peking Union Medical College Hospital | February 1, 2023 | Phase 2 |
NCT05130827 | Active, not recruiting | Drug: Plinabulin | Multiple Myeloma | Memorial Sloan Kettering Cancer Center |
December 21, 2021 | Phase 2 |
NCT02812667 | Active, not recruiting | Drug: Nivolumab + Plinabulin | Non-small Cell Lung Cancer Metastatic |
Lyudmila Bazhenova, M.D. | August 29, 2016 | Phase 1 |
NCT03294577 | Active, not recruiting | Drug: Pegfilgrastim Drug: Plinabulin |
Chemotherapy-induced Neutropenia | BeyondSpring Pharmaceuticals Inc. | October 23, 2019 | Phase 3 |