Plinabulin (Synonyms: 普那布林; NPI-2358)

目录号: HY-14444 纯度: ≥98.0%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Plinabulin (NPI-2358) 是一种抗微管蛋白解聚的血管破坏剂，能结合 β-微管蛋白 (β-tubulin) 的秋水仙碱结合位点阻止聚合，并且对人肿瘤细胞系具有抑制作用，对 HT-29 细胞系的 IC₅₀ 值为 9.8 nM。

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Plinabulin Chemical Structure

CAS No. : 714272-27-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1377	In-stock
1 mg	￥569	In-stock
5 mg	￥1252	In-stock
10 mg	￥2358	In-stock
50 mg	现货	询价
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

Other Forms of Plinabulin:

Plinabulin-d₁ 询价

Plinabulin 相关产品

•相关化合物库:

•同靶点产品:

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生物活性
纯度 & 产品资料
参考文献

生物活性

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]

细胞效力
(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]

体外研究
(In Vitro)

PlinabuLin (NPI-2358) (2 -200 nM；30 分钟；HUVECs 细胞) 是一种有效的抗肿瘤剂，在多重耐药 (MDR) 肿瘤细胞系中具有活性，能够快速诱导微管蛋白解聚和单层通透性在 HUVEC 中，DU 145 细胞的 IC₅₀ 值为 18 nM；PC-3 细胞为 13 nM；MDA-MB-231 细胞为 14 nM；NCI-H292 细胞为 18 nM；Jurkat 白血病细胞为 11 nM^[1]。

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.

体内研究
(In Vivo)

PlinabuLin (0 mg/kg-15 mg/kg；腹膜内注射；雌性 CDF1 和 C3H/He 小鼠) 诱导肿瘤灌注的时间和剂量依赖性降低。KHT 肉瘤比 C3H 肿瘤对 Plinabulin 的抗肿瘤作用更敏感，而两种模型的放射反应均得到增强^[3]。

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

分子量

336.39

Formula

C₁₉H₂₀N₄O₂

CAS 号

714272-27-2

性状

固体

颜色

Light yellow to yellow

中文名称

普那布林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (148.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.43 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.43 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: ≥98.0%

选择批次：

Data Sheet (630 KB) SDS (251 KB)

COA (199 KB) HNMR (247 KB)

产品使用指南 (1538 KB)

参考文献

[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]

Plinabulin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

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-2358普那布林NPI2358NPI 2358Microtubule/TubulinInhibitorinhibitorinhibit

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Plinabulin (Synonyms: 普那布林; NPI-2358)

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完整储备液配制表

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Plinabulin (Synonyms: 普那布林; NPI-2358)

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摩尔计算器

稀释计算器

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