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Plinabulin
🥰Excellent
Catalog No. T2511Cas No. 714272-27-2
Alias NPI-2358
Plinabulin (NPI-2358) (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing tumor cells ( IC50: 9.8-18 nM). Plinabulin selectively targets and binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics. This disrupts mitotic spindle assembly leading to cell cycle arrest at M phase and blockage of cell division.
Plinabulin
🥰Excellent
Purity: 100%
Catalog No. T2511Alias NPI-2358Cas No. 714272-27-2
Plinabulin (NPI-2358) (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing tumor cells ( IC50: 9.8-18 nM). Plinabulin selectively targets and binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics. This disrupts mitotic spindle assembly leading to cell cycle arrest at M phase and blockage of cell division.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $33 | In Stock | |
| 5 mg | $52 | In Stock | |
| 10 mg | $77 | In Stock | |
| 25 mg | $143 | In Stock | |
| 50 mg | $231 | In Stock | |
| 100 mg | $369 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $57 | In Stock |
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CitedSelect Batch
Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Plinabulin (NPI-2358) (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing tumor cells ( IC50: 9.8-18 nM). Plinabulin selectively targets and binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics. This disrupts mitotic spindle assembly leading to cell cycle arrest at M phase and blockage of cell division. |
| Targets&IC50 | Tubulin:9.8 nM-18 nM |
| In vitro | NPI-2358 induces a reduction in tumor perfusion in a time- and dose-dependent manner. In mice carrying human plasmacytoma xenografts, NPI-2358 (7.5 mg/kg) significantly inhibits tumor growth. Compared to its efficacy in C3H tumors, NPI-2358 demonstrates superior activity against KHT sarcomas, and its anticancer effectiveness is enhanced when combined with radiation therapy. |
| In vivo | In human umbilical vein endothelial cells, NPI-2358 (20 nM) rapidly induces the depolymerization of microtubule proteins and penetrates the monolayer of cells. It arrests MM cells in the early phases of mitosis and induces cell death. NPI-2358 binds to the colchicine binding site of microtubule proteins, effectively inhibiting human tumor cell lines that overexpress Pgp, or reducing the catalytic activity of nuclear Topo II (IC50: 9.8-18 nM). Moreover, it inhibits microtubule formation and the migration of endothelial and MM cells, leading to dysfunction in the tumor vasculature. NPI-2358 induces mitotic arrest or death in MM cells, but this effect can be deactivated by blocking the JNK pathway. |
| Cell Research | The adherent cells are plated in 96-well flat-bottomed plates and allowed to attach for 24 hours at 37 °C. HL-60 and HL-60/MX2 cells are plated in 96-well plates on the day of NPI-2358 addition. Serially diluted NPI-2358 is added to cells at concentrations ranging from 2 pM to 20 μM. Cells treated with a final concentration of 0.25% (v/v) DMSO serves as the vehicle control. Cell viability is assessed 48 hours later by measuring the reduction of resazurin with a fluorimeter. The IC50 value is calculated.(Only for Reference) |
| Alias | NPI-2358 |
| Molecular Weight | 336.39 |
| Formula | C19H20N4O2 |
| Cas No. | 714272-27-2 |
| Smiles | CC(C)(C)c1[nH]cnc1C=c1[nH]c(=O)c(=Cc2ccccc2)[nH]c1=O |
| Relative Density. | 1.267 g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (148.6 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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