1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin
  3. Plinabulin

Plinabulin (Synonyms: NPI-2358)

Cat. No.: HY-14444
Handling Instructions

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.

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Plinabulin Chemical Structure

Plinabulin Chemical Structure

CAS No. : 714272-27-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 280 In-stock
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100 mg USD 450 In-stock
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Description

Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells[1]. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells[2].

In Vitro

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].

Cell Viability Assay[1]

Cell Line: HUVECs cells
Concentration: 2 nM, 10 nM, 20 nM and 200 nM
Incubation Time: 30 minutes
Result: Low concentrations (2 nM, 10 nM) rapidly induced tubulin depolymerization in HUVECs.
In Vivo

Plinabulin (0 mg/kg-15 mg/kg; intraperitoneal injection; female CDF1 and C3H/He mice) induces a time- and dose-dependent decrease in tumor perfusion. The KHT sarcoma is more sensitive than the C3H tumor to the anti-tumor effects of Plinabulin, while radiation response is enhanced in both models[3].

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]
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
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.
Molecular Weight

336.39

Formula

C₁₉H₂₀N₄O₂

CAS No.

714272-27-2

SMILES

O=C(N/C1=C\C2=C(NC=N2)C(C)(C)C)/C(NC1=O)=C/C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (148.64 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Plinabulin
Cat. No.:
HY-14444
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