Plinabulin (NPI-2358)

Catalog No.S1176

For research use only.

Plinabulin (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.

Plinabulin (NPI-2358) Chemical Structure

CAS No. 714272-27-2

Selleck's Plinabulin (NPI-2358) has been cited by 5 Publications

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Biological Activity

Description Plinabulin (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.
Features Synthetic analog of NPI-2350 and greater potentcy than NPI-2350.
Targets
Tubulin [1]
9.8 nM-18 nM
In vitro

NPI-2358 binds to the colchicine-binding site of tubulin and has potent inhibitory to human tumor cell lines which have overexpressed Pgp or reduced nuclear Topo II catalytic activity, with IC50 from 9.8 to 18 nM. NPI-2358 is able to rapidly induce tubulin depolymerization in HUVECs and monolayer permeability even at 20 nM. [1] NPI-2358 induces cell death in MM cells with IC50 of 8-10 nM, which due to trigger early mitotic arrest in MM cells. NPI-2358 also inhibits tubule formation and migration of endothelial as well as MM cells, which leads to disrupt tumor vasculature. NPI-2358 could induces cell death in patient MM (CD138+) cells without effecting viability of normal mononuclear cells. Blockade of JNK abrogates NPI-2358-induced mitotic arrest or MM cell death. [2]

In vivo NPI-2358 (7.5 mg/kg) inhibits tumor growth in human plasmacytoma mouse xenograft models at well-tolerated doses. [2] NPI-2358 induces a time- and dose-dependent decrease in tumour perfusion. NPI-2358 is more sensitive to the KHT sarcoma than the C3H tumour, while radiation response could enhance the antitumor activity in both models. [3]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: HT-29, PC-3, DU 145, MDA-MB-231, NCI-H292, Jurkat, MES-SA, MES-SA/Dx5, HL-60, HL-60/MX2.
  • Concentrations: 2 pM - 20 μM
  • Incubation Time: 24 hours.
  • Method: 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.
Animal Research:[3]
  • Animal Models: CDF1 mice or C3H/Hej mice.
  • Dosages: ~15 mg/kg.
  • Administration: Injected intraperitoneally (i.p.) in a volume of 0.02 mL/g mouse body weight in CDF1 mice and 0.01 mL/g body weight for C3H/Hej mice.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 336.39
Formula

C19H20N4O2

CAS No. 714272-27-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)C1=C(N=CN1)C=C2C(=O)NC(=CC3=CC=CC=C3)C(=O)N2

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02846792 Terminated Biological: Nivolumab|Drug: Plinabulin ALK Gene Translocation|EGFR Activating Mutation|Recurrent Non-Small Cell Lung Carcinoma|ROS1 Gene Translocation|Stage IIIB Non-Small Cell Lung Cancer AJCC v7|Stage IV Non-Small Cell Lung Cancer AJCC v7 University of Washington|National Cancer Institute (NCI) June 14 2017 Phase 1|Phase 2
NCT00630110 Completed Drug: docetaxel|Drug: NPI-2358 + docetaxel Cancer Nereus Pharmaceuticals Inc. February 2008 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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