Plinabulin (NPI-2358)

Alias: NPI-2358; Plinabulin; NPI2358; NPI 2358;
Cat No.:V0683 Purity: ≥98%
Plinabulin (formerly also known as NPI-2358) is a novel and potent vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.
Plinabulin (NPI-2358) Chemical Structure CAS No.: 714272-27-2
Product category: VDA
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Plinabulin (formerly also known as NPI-2358) is a novel and potent vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. It demonstrate significant in vivo antitumor efficacy in human plasmacytoma mouse xenograft models. Plinabulin is a first-in-class and selective immunomodulating microtubule-binding agent (SIMBA), which binds in the vicinity of the colchicine binding domain of tubulin.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
PlinabuLin (NPI-2358), a potent antineoplastic agent, rapidly induces tubulin depolymerization and monolayer permeability in multidrug-resistant (MDR) tumor cell lines. In HUVEC, the IC50 values are 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 for Jurkat leukemia cells. nM[1].
ln Vivo
Tumor perfusion is reduced in a dose- and time-dependent manner in female CDF1 and C3H/He mice when given plinabuLin (0 mg/kg–15 mg/kg; intraperitoneally). Plinabulin's anticancer effects are more responsive to KHT sarcomas than they are to C3H tumors, and both models exhibit an increased radiation response [3].
Cell Assay
Cell Viability Assay[1]
Cell Types: HUVECs cells
Tested Concentrations: 2 nM, 10 nM, 20 nM and 200 nM
Incubation Duration: 30 minutes
Experimental Results: Low concentrations (2 nM, 10 nM) rapidly induced tubulin depolymerization in HUVECs.
Animal Protocol
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.
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.
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H20N4O2
Molecular Weight
336.39
CAS #
714272-27-2
SMILES
O=C(/C(NC/1=O)=C\C2=CC=CC=C2)NC1=C\C3=C(C(C)(C)C)NC=N3
Chemical Name
(3E,6E)-3-benzylidene-6-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)piperazine-2,5-dione
Synonyms
NPI-2358; Plinabulin; NPI2358; NPI 2358;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 54 mg/mL (160.5 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • Plinabulin (NPI-2358)

    Antivascular activity of plinabulin.Blood.2011 May 26;117(21):5692-700.

  • Plinabulin (NPI-2358)

    Cell death induced by plinabulin depends on JNK as well as caspases.Blood.2011 May 26;117(21):5692-700.

  • Plinabulin (NPI-2358)

    Plinabulin inhibits growth and triggers apoptosis in MM.Blood.2011 May 26;117(21):5692-700.

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