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 agents (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.

For research use only. We do not sell to patients.

Plinabulin Chemical Structure

Plinabulin Chemical Structure

CAS No. : 714272-27-2

Size Price Stock Quantity
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
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Plinabulin (NPI-2358) is a vascular disrupting agents (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. IC50 Value: 9.8~18 nM Target: Microtubule/Tubulin 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. 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. in vivo: NPI-2358 (7.5 mg/kg) inhibits tumor growth in human plasmacytoma mouse xenograft models at well-tolerated doses. 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.

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% corn oil

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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
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

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Product Name:
Plinabulin
Cat. No.:
HY-14444
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Plinabulin

Cat. No.: HY-14444