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Plinabulin

Plinabulin

Item no.	S1176-200
Manufacturer	Selleckchem
CASRN	714272-27-2
Amount	200 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 200 mg 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Skin Cancer Lymphatic System Cancer Bone Cancer
Type	Inhibitors
Specific against	other
Smiles	CC(C)(C)C1=C(N=CN1)C=C2C(=O)NC(=CC3=CC=CC=C3)C(=O)N2
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	NPI-2358
Similar products	NPI-2358
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	336, 39
Administration	Injected intraperitoneally (i.p.) in a volume of 0.02 mL/g mouse body weight in CDF1 mice and 0.01 mL/g body weight for C3H/Hej mice.
Animal Models	CDF1 mice or C3H/Hej mice.
Cell lines	HT-29, PC-3, DU 145, MDA-MB-231, NCI-H292, Jurkat, MES-SA, MES-SA/Dx5, HL-60, HL-60/MX2.
Clinical Trials	Phase I has been completed in patients with advanced solid tumor malignancies or lymphoma.
Concentrations	2 pM - 20 uM
Dosages	ca.15 mg/kg.
Formulation	Freshly prepared in a polyethylene glycol/solutol solution and diluted to the required concentration with 5% dextrose.
IC50	9.8ca.18 nM [1], 9.8ca.18 nM [1], 9.8ca.18 nM [1], 9.8ca.18 nM [1], 9.8ca.18 nM [1], 9.8ca.18 nM [1]
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. [1] 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. [2]
In vivo	NPI-2358 (7.5 mg/kg) inhibits tumor growth in human plasmacytoma mouse xenograft models at well-tolerated doses. [2] 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. [3]
Incubation Time	24 hours.
Method	The adherent cells are plated in 96-well flat-bottomed plates and allowed to attach for 24 hours at 37 C. HL-60 and HL-60/MX2 cells are plated in 96-well plates on the day of NPI-2358 addition. Serially diluted NPI-2358 is added to cells at concentrations ranging from 2 pM to 20 uM. Cells treated with a final concentration of 0.25% (v/v) DMSO serves as the vehicle control. Cell viability is assessed 48 hours later by measuring the reduction of resazurin with a fluorimeter. The IC50 value is calculated.
Solubility (25C)	DMSO 67 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.
Chemical Name	(3Z, 6Z)-3-benzylidene-6-((5-tert-butyl-1H-imidazol-4-yl)methylene)piperazine-2, 5-dione
Features	Synthetic analog of NPI-2350 and More potent than NPI-2350

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

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S1176-200-datasheet.pdf

S1176-200-safety-datasheet.pdf