[CAS NO. 714272-27-2] Plinabulin (NPI-2358)
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PRODUCTS SPECIFICATIONS [714272-27-2]
Store
Catalog
SLK-S1176
Brand
Selleck
CAS
714272-27-2
DESCRIPTION [714272-27-2]
Overview
| MDL | MFCD18074510 |
|---|---|
| Molecular Weight | 336.39 |
| Molecular Formula | C19H20N4O2 |
| SMILES | C(\C1=C(C(C)(C)C)N=CN1)=C\2/C(=O)N/C(=C\C3=CC=CC=C3)/C(=O)N2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
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 |
| 50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL |
Description
Plinabulin (NPI-2358) is a against tubulin-depolymerizing with of 9.8~18 nM in tumor cells. Phase 1/2.
Features
Synthetic analog of NPI-2350 and greater potentcy than NPI-2350.
Targets
| Tubulin [1] |
| 9.8 nM-18 nM |
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.
References
Synonyms
2,5-Piperazinedione, 3-[[5-(1,1-dimethylethyl)-1H-imidazol-4-yl]methylene]-6-(phenylmethylene)-, (3Z,6Z)-
(3Z,6Z)-3-[[5-(1,1-Dimethylethyl)-1H-imidazol-4-yl]methylene]-6-(phenylmethylene)-2,5-piperazinedione
NPI 2358
Plinabulin
BPI 2358
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