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Plinabulin

Catalog No. T2511 CAS 714272-27-2

Synonyms: NPI-2358

Plinabulin (NPI-2358) (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing tumor cells ( IC50: 9.8-18 nM). Plinabulin selectively targets and binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics. This disrupts mitotic spindle assembly leading to cell cycle arrest at M phase and blockage of cell division.

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Plinabulin, CAS 714272-27-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 143.00
50 mg	In stock	$ 231.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 100%

Purity: 98.69%

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Chemical Properties

Storage & Solubility Information

Description	Plinabulin (NPI-2358) (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing tumor cells ( IC50: 9.8-18 nM). Plinabulin selectively targets and binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics. This disrupts mitotic spindle assembly leading to cell cycle arrest at M phase and blockage of cell division.
Targets&IC50	Tubulin:9.8 nM-18 nM
In vitro	NPI-2358 induces a reduction in tumor perfusion in a time- and dose-dependent manner. In mice carrying human plasmacytoma xenografts, NPI-2358 (7.5 mg/kg) significantly inhibits tumor growth. Compared to its efficacy in C3H tumors, NPI-2358 demonstrates superior activity against KHT sarcomas, and its anticancer effectiveness is enhanced when combined with radiation therapy.
In vivo	In human umbilical vein endothelial cells, NPI-2358 (20 nM) rapidly induces the depolymerization of microtubule proteins and penetrates the monolayer of cells. It arrests MM cells in the early phases of mitosis and induces cell death. NPI-2358 binds to the colchicine binding site of microtubule proteins, effectively inhibiting human tumor cell lines that overexpress Pgp, or reducing the catalytic activity of nuclear Topo II (IC50: 9.8-18 nM). Moreover, it inhibits microtubule formation and the migration of endothelial and MM cells, leading to dysfunction in the tumor vasculature. NPI-2358 induces mitotic arrest or death in MM cells, but this effect can be deactivated by blocking the JNK pathway.
Cell Research	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 μM. 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.(Only for Reference)

Synonyms	NPI-2358
Molecular Weight	336.39
Formula	C19H20N4O2
CAS No.	714272-27-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (148.6 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Nicholson B, et al. Anticancer Drugs, 2006, 17(1), 25-31. 2. Singh AV, et al. Blood, 2011, 117(21), 5692-5700. 3. Bertelsen LB, et al. Int J Radiat Biol, 2011, 87(11), 1126-1134.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Inhibitor Library Microtubule-Targeted Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Breast Cancer Compound Library Anti-Aging Compound Library Anti-Lung Cancer Compound Library Clinical Compound Library

Related Products

Related compounds with same targets

2-Methoxyestradiol Jasplakinolide Albendazole Vinblastine BNC105 Taccalonolide A Glembatumumab vedotin Colchicine

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Keywords

Plinabulin 714272-27-2 Cytoskeletal Signaling Microtubule Associated NPI2358 inhibit Inhibitor Microtubule/Tubulin NPI 2358 NPI-2358 inhibitor

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