Plinabulin (Synonyms: NPI-2358)

Name: Plinabulin
Brand: MedChemExpress
SKU: HY-14444
Rating: 4.5 (1 reviews)

Cat. No.: HY-14444 Purity: ≥98.0%: FAQs
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Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC₅₀ of 9.8 nM against HT-29 cells. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells.

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Plinabulin Chemical Structure

CAS No. : 714272-27-2

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10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Plinabulin:

Plinabulin-d₁ Get quote

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Description

Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC₅₀ of 9.8 nM against HT-29 cells^[1]. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells^[2].

IC₅₀ & Target

β-tubulin^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.0055 μM Compound: NPI-2358	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
A549	IC₅₀	0.01 μM Compound: Plinabulin	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
A549	IC₅₀	3.5 nM Compound: Plinabulin	Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30910474]
A549	IC₅₀	35.7 nM Compound: 1	Cytotoxicity against human A549 cells after 48 hrs by WST8 assay Cytotoxicity against human A549 cells after 48 hrs by WST8 assay	[PMID: 25313318]
BGC-823	IC₅₀	0.009 μM Compound: Plinabulin	Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
BXPC-3	IC₅₀	4.28 nM Compound: Plinabulin	Antiproliferative activity against human BxPC3 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human BxPC3 cells after 72 hrs by sulforhodamine B assay	[PMID: 29571653]
BXPC-3	IC₅₀	5.8 nM Compound: Plinabulin	Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32278711]
DU-145	IC₅₀	0.014 μM Compound: NPI-2358	Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
HCT-116	IC₅₀	6 nM Compound: Plinabulin	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
HeLa	IC₅₀	0.0084 μM Compound: NPI-2358	Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
HeLa	IC₅₀	0.01 μM Compound: Plinabulin	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
HeLa	IC₅₀	20.6 nM Compound: 1	Cytotoxicity against human HeLa cells after 48 hrs by WST8 assay Cytotoxicity against human HeLa cells after 48 hrs by WST8 assay	[PMID: 25313318]
HeLa	IC₅₀	9 nM Compound: Plinabulin	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
HepG2	IC₅₀	4.8 nM Compound: Plinabulin	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
HL-60	IC₅₀	0.01 μM Compound: Plinabulin	Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
HL-60	IC₅₀	0.0148 μM Compound: NPI-2358	Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
HT-29	IC₅₀	0.013 μM Compound: NPI-2358	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
HT-29	IC₅₀	13.5 nM Compound: 1, NPI-2358, KPU-2	Cytotoxicity against human HT-29 cells after 72 hrs by XTT/PMS method Cytotoxicity against human HT-29 cells after 72 hrs by XTT/PMS method	[PMID: 21106379]
HT-29	IC₅₀	14.9 nM Compound: 11, KPU-2/NPI-2358, Plinabulin	Cytotoxicity against human HT-29 cells after 48 hrs using resazurin by microplate fluorometer analysis Cytotoxicity against human HT-29 cells after 48 hrs using resazurin by microplate fluorometer analysis	[PMID: 22185476]
HT-29	IC₅₀	15 nM Compound: 3, NPI-2358/KPU-2	Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay	[PMID: 22727370]
HT-29	IC₅₀	6.6 nM Compound: Plinabulin	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32278711]
Huh-7	IC₅₀	0.031 μM Compound: Plinabulin	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
HUVEC	IC₅₀	11 nM Compound: 11, KPU-2/NPI-2358, Plinabulin	Cytotoxicity against HUVEC after 48 hrs using resazurin by microplate fluorometer analysis Cytotoxicity against HUVEC after 48 hrs using resazurin by microplate fluorometer analysis	[PMID: 22185476]
Jurkat	IC₅₀	3.3 nM Compound: Plinabulin	Cytotoxicity against human Jurkat cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28228362]
K562	IC₅₀	0.0063 μM Compound: NPI-2358	Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
K562	IC₅₀	0.008 μM Compound: Plinabulin	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
MCF7	IC₅₀	0.01 μM Compound: Plinabulin	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
MCF7	IC₅₀	0.0126 μM Compound: NPI-2358	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]
MCF7	IC₅₀	29.8 nM Compound: Plinabulin	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
NCI-H1975	IC₅₀	0.011 μM Compound: Plinabulin	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
NCI-H1975	IC₅₀	10.2 nM Compound: Plinabulin	Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30910474]
NCI-H446	IC₅₀	44.2 nM Compound: Plinabulin	Cytotoxicity against human NCI-H446 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human NCI-H446 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28228362]
NCI-H460	IC₅₀	26.2 nM Compound: Plinabulin	Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32278711]
NCI-H460	IC₅₀	26.2 nM Compound: Plinabulin	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
NCI-H460	IC₅₀	33.9 nM Compound: Plinabulin	Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28228362]
U-937	IC₅₀	0.006 μM Compound: Plinabulin	Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 24960627]
U-937	IC₅₀	0.0068 μM Compound: NPI-2358	Cytotoxicity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 27318124]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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.

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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female CDF1 mice (10-14-week-old) with C3H mammary carcinoma; Female C3H/HeJ mice with KHT sarcoma cells (8-weeks-old)^[3]
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.

Clinical Trial

Molecular Weight

336.39

Formula

C₁₉H₂₀N₄O₂

CAS No.

714272-27-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N/C1=C\C2=C(NC=N2)C(C)(C)C)/C(NC1=O)=C/C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (148.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.43 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (254 KB) HNMR (247 KB)

Handling Instructions (2659 KB)

References

[1]. Nicholson B et al. NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Anticancer Drugs. 2006 Jan;17(1):25-31. [Content Brief]

[2]. Monica M. Mita et al. Phase 1 First-in-Human Trial of the Vascular Disrupting Agent Plinabulin (NPI-2358) in Patients with Solid Tumors or Lymphomas Clin Cancer Res. 2010 Dec 1;16(23):5892-9. [Content Brief]

[3]. Bertelsen LB, et al. Vascular effects of plinabulin (NPI-2358) and the influence on tumour response when given alone or combined with radiation. Int J Radiat Biol. 2011 Nov;87(11):1126-34. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9727 mL	14.8637 mL	29.7274 mL	74.3185 mL
	5 mM	0.5945 mL	2.9727 mL	5.9455 mL	14.8637 mL
	10 mM	0.2973 mL	1.4864 mL	2.9727 mL	7.4318 mL
	15 mM	0.1982 mL	0.9909 mL	1.9818 mL	4.9546 mL
	20 mM	0.1486 mL	0.7432 mL	1.4864 mL	3.7159 mL
	25 mM	0.1189 mL	0.5945 mL	1.1891 mL	2.9727 mL
	30 mM	0.0991 mL	0.4955 mL	0.9909 mL	2.4773 mL
	40 mM	0.0743 mL	0.3716 mL	0.7432 mL	1.8580 mL
	50 mM	0.0595 mL	0.2973 mL	0.5945 mL	1.4864 mL
	60 mM	0.0495 mL	0.2477 mL	0.4955 mL	1.2386 mL
	80 mM	0.0372 mL	0.1858 mL	0.3716 mL	0.9290 mL
	100 mM	0.0297 mL	0.1486 mL	0.2973 mL	0.7432 mL

Plinabulin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Plinabulin714272-27-2NPI-2358NPI2358NPI 2358Microtubule/TubulinInhibitorinhibitorinhibit

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Plinabulin (Synonyms: NPI-2358)

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