Plinabulin

SKU: orb1224168

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.(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.(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.

Key Properties

• CAS Number: 714272-27-2
• MW: 336.39
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₀N₄O₂
• SMILES: O=C(/C(NC/1=O)=C\C2=CC=CC=C2)NC1=C\C3=C(C(C)(C)C)NC=N3
• Target: Microtubule/Tubulin
• Solubility: DMSO: 54 mg/mL warmed (160.52 mM)

Bioactivity

• In Vivo:
  Animal model: Female CDF1 mice (10-14-week-old) with C3H mammary carcinoma; Female C3H/HeJ mice with KHT sarcoma cells (8-weeks-old). 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.
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• In Vitro:
  Cell Viability Assay 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NPI-2358

Quick Database Links

Gene Symbol

Microtubule/Tubulin