Plinabulin (NPI-2358) is a vascular disrupting agents(VDA) against tubulin depolymerization with IC50 of 9.8~18 nM in tumor cells. Disrupting tubulin depolymerization with IC50 of 1/2. Phase 1/2. NPI-2358 is a synthetic of NPI-2350 and is more effective than NPI-2350.

 

Brand: BCM

 

Solubility: Soluble in DMSO (warmed with 50ºC water bath). Insoluble in Water; insoluble in Ethanol.

 

InChIKey: UNRCMCRRFYFGFX-TYPNBTCFSA-N

 

Mechanism of Action: NPI-2358 is a vascular disrupting agent currently in clinical development for the treatment of cancer by Nereus. NPI-2358 is one of over 200 synthetic analogues that were prepared following the discovery of the compound Halimide isolated from a marine fungus. In preclinical models of cancer, including lung, breast, sarcoma, colon and prostate, NPI-2358 demonstrated potent and selective anti-tumor effects in combination with docetaxel and other oncology therapies, as well as single-agent efficacy in a number of orthotopic models. NPI-2358 interacts with soluble beta-tubulin and prevents the polymerization of tubulin without altering dynamic microtubule function of formed microtubules. As demonstrated in preclinical testing, this target profile results in a highly specific nanomolar cytotoxicity while reducing the side effects seen in first-generation VDAs due to cardiotoxicity, hemodynamic changes and neuropathies.

 

Attribute
[CAS No.]	714272-27-2
[Formula]	C19H20N4O2
[Molecular]	336.39
[Chem Name]	(3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]piperazine-2,5-dione
[Synonym]	Plinabulin; NPI-2358
[Storage]	Sealed in dry. Stored under -20°C.
[MDL No.]	MFCD18074510
[Form]	Powder

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