Plinabulin
Based on 3 publication(s) in Google Scholar
Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 714272-27-2
- Formula: C19H20N4O2
- Molecular Weight:336.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Plinabulin
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Biological Activity
β-tubulin[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.0055 μM
Compound: NPI-2358
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| A549 | IC50 |
0.01 μM
Compound: Plinabulin
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| A549 | IC50 |
3.5 nM
Compound: Plinabulin
|
Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 30910474] |
| A549 | IC50 |
35.7 nM
Compound: 1
|
Cytotoxicity against human A549 cells after 48 hrs by WST8 assay
Cytotoxicity against human A549 cells after 48 hrs by WST8 assay
|
[PMID: 25313318] |
| BGC-823 | IC50 |
0.009 μM
Compound: Plinabulin
|
Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| BXPC-3 | IC50 |
18.4 nM
Compound: Plinabulin
|
Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition by MTT assay
|
[PMID: 37301522] |
| BXPC-3 | IC50 |
4.28 nM
Compound: Plinabulin
|
Antiproliferative activity against human BxPC3 cells after 72 hrs by sulforhodamine B assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 29571653] |
| BXPC-3 | IC50 |
5.8 nM
Compound: Plinabulin
|
Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 32278711] |
| DU-145 | IC50 |
0.014 μM
Compound: NPI-2358
|
Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| HCT-116 | IC50 |
6 nM
Compound: Plinabulin
|
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 31759826] |
| HCT-116 | IC50 |
8.8 nM
Compound: Plinabulin
|
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition by MTT assay
|
[PMID: 37301522] |
| HeLa | IC50 |
0.0084 μM
Compound: NPI-2358
|
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| HeLa | IC50 |
0.01 μM
Compound: Plinabulin
|
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| HeLa | IC50 |
20.6 nM
Compound: 1
|
Cytotoxicity against human HeLa cells after 48 hrs by WST8 assay
Cytotoxicity against human HeLa cells after 48 hrs by WST8 assay
|
[PMID: 25313318] |
| HeLa | IC50 |
9 nM
Compound: Plinabulin
|
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 31759826] |
| HepG2 | IC50 |
4.8 nM
Compound: Plinabulin
|
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 31759826] |
| HL-60 | IC50 |
0.01 μM
Compound: Plinabulin
|
Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| HL-60 | IC50 |
0.0148 μM
Compound: NPI-2358
|
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| HT-29 | IC50 |
0.013 μM
Compound: NPI-2358
|
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| HT-29 | IC50 |
13.5 nM
Compound: 1, NPI-2358, KPU-2
|
Cytotoxicity against human HT-29 cells after 72 hrs by XTT/PMS method
Cytotoxicity against human HT-29 cells after 72 hrs by XTT/PMS method
|
[PMID: 21106379] |
| HT-29 | IC50 |
14.9 nM
Compound: 11, KPU-2/NPI-2358, Plinabulin
|
Cytotoxicity against human HT-29 cells after 48 hrs using resazurin by microplate fluorometer analysis
Cytotoxicity against human HT-29 cells after 48 hrs using resazurin by microplate fluorometer analysis
|
[PMID: 22185476] |
| HT-29 | IC50 |
15 nM
Compound: 3, NPI-2358/KPU-2
|
Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay
Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay
|
[PMID: 22727370] |
| HT-29 | IC50 |
15 nM
Compound: 1, NPI-2358/KPU-2
|
Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
|
[PMID: 20395148] |
| HT-29 | IC50 |
18 nM
Compound: NPI-2358
|
Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
|
[PMID: 21835627] |
| HT-29 | IC50 |
6.6 nM
Compound: Plinabulin
|
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 32278711] |
| Huh-7 | IC50 |
0.031 μM
Compound: Plinabulin
|
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| HUVEC | IC50 |
10 nM
Compound: Plinabulin
|
Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth
Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth
|
[PMID: 30542530] |
| HUVEC | IC50 |
11 nM
Compound: 11, KPU-2/NPI-2358, Plinabulin
|
Cytotoxicity against HUVEC after 48 hrs using resazurin by microplate fluorometer analysis
Cytotoxicity against HUVEC after 48 hrs using resazurin by microplate fluorometer analysis
|
[PMID: 22185476] |
| Jurkat | IC50 |
3.3 nM
Compound: Plinabulin
|
Cytotoxicity against human Jurkat cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as decrease in cell viability after 72 hrs by MTT assay
|
[PMID: 28228362] |
| K562 | IC50 |
0.0063 μM
Compound: NPI-2358
|
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| K562 | IC50 |
0.008 μM
Compound: Plinabulin
|
Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| MCF7 | IC50 |
0.01 μM
Compound: Plinabulin
|
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| MCF7 | IC50 |
0.0126 μM
Compound: NPI-2358
|
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
| MCF7 | IC50 |
29.8 nM
Compound: Plinabulin
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 31759826] |
| NCI-H1975 | IC50 |
0.011 μM
Compound: Plinabulin
|
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| NCI-H1975 | IC50 |
10.2 nM
Compound: Plinabulin
|
Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 30910474] |
| NCI-H446 | IC50 |
44.2 nM
Compound: Plinabulin
|
Cytotoxicity against human NCI-H446 cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human NCI-H446 cells assessed as decrease in cell viability after 72 hrs by MTT assay
|
[PMID: 28228362] |
| NCI-H460 | IC50 |
26.2 nM
Compound: Plinabulin
|
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 31759826] |
| NCI-H460 | IC50 |
26.2 nM
Compound: Plinabulin
|
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 32278711] |
| NCI-H460 | IC50 |
30.9 nM
Compound: Plinabulin
|
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
|
[PMID: 37301522] |
| NCI-H460 | IC50 |
33.9 nM
Compound: Plinabulin
|
Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 72 hrs by MTT assay
|
[PMID: 28228362] |
| U-937 | IC50 |
0.006 μM
Compound: Plinabulin
|
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
|
[PMID: 24960627] |
| U-937 | IC50 |
0.0068 μM
Compound: NPI-2358
|
Cytotoxicity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
|
[PMID: 27318124] |
Plinabulin (NPI-2358) (2-200 nM; 30 minutes; HUVECs cells) is a potent anti-tumor agent which is active in multidrug-resistant (MDR) tumor cell lines, and is able to rapidly induce tubulin depolymerization and monolayer permeability in HUVECs, with IC50 values of 18 nM for DU 145 cells; 13 nM for PC-3 cells; 14 nM for MDA-MB-231 cells; 18 nM for NCI-H292 cells; and 11 nM for Jurkat leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVECs cells
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Concentration:2 nM, 10 nM, 20 nM and 200 nM
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Incubation Time:30 minutes
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Result:Low concentrations (2 nM, 10 nM) rapidly induced tubulin depolymerization in HUVECs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CDF1 mice (10-14-week-old) with C3H mammary carcinoma; Female C3H/HeJ mice with KHT sarcoma cells (8-weeks-old)[3]
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Dosage: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 -
Administration:Intraperitoneal injection; 0 huor, 1 huor, 3 hours, 6 huors, 24 huors
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Result: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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 714272-27-2
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Appearance Solid
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Molecular Weight 336.39
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Formula C19H20N4O2
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Color Light yellow to yellow
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SMILES
O=C(N/C1=C\C2=C(NC=N2)C(C)(C)C)/C(NC1=O)=C/C3=CC=CC=C3
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Synonyms
NPI-2358
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Clin Transl Med
Mechanism of Gzma-mediated GEF-H1 activation in intestinal epithelial cells leading to intestinal barrier dysfunction in sepsis. [Abstract]2026 Apr;16(4):e70651. PMID: 41943423 -
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bioRxiv
Diverse microtubule-destabilizing drugs induce equivalent molecular pathway responses in endothelial cells. [Abstract]2025 Jan 24:2025.01.22.632572. PMID: 39896568
Solvent & Solubility
DMSO : 50 mg/mL (148.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.43 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9727 mL | 14.8637 mL | 29.7274 mL | 74.3185 mL |
| 5 mM | 0.5945 mL | 2.9727 mL | 5.9455 mL | 14.8637 mL | |
| 10 mM | 0.2973 mL | 1.4864 mL | 2.9727 mL | 7.4318 mL | |
| 15 mM | 0.1982 mL | 0.9909 mL | 1.9818 mL | 4.9546 mL | |
| 20 mM | 0.1486 mL | 0.7432 mL | 1.4864 mL | 3.7159 mL | |
| 25 mM | 0.1189 mL | 0.5945 mL | 1.1891 mL | 2.9727 mL | |
| 30 mM | 0.0991 mL | 0.4955 mL | 0.9909 mL | 2.4773 mL | |
| 40 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8580 mL | |
| 50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4864 mL | |
| 60 mM | 0.0495 mL | 0.2477 mL | 0.4955 mL | 1.2386 mL | |
| 80 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
| 100 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL |