Plinabulin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Plinabulin (NPI-2358) 是一种抗微管蛋白解聚的血管破坏剂 (VDA)，在肿瘤细胞中的 IC50 为 9.8~18 nM。阶段 1/2。

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.

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.

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.

NPI-2358

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Tubulin

Cancer

——

714272-27-2

336.39

C19H20N4O2

>98% (HPLC)

DMSO: 54 mg/mL warmed (160.52 mM)

O=C(/C(NC/1=O)=C\C2=CC=CC=C2)NC1=C\C3=C(C(C)(C)C)NC=N3

(3E,6E)-3-benzylidene-6-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)piperazine-2,5-dione

(-20℃)

With Ice Pack

≥ 2 years