Volasertib (Synonyms: 伏拉塞替; BI 6727)

目录号: HY-12137 纯度: 99.41%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Volasertib (BI 6727) 是一种具有口服活性的、高效的、ATP 竞争性的 Polo 样激酶 1 (PLK1) 抑制剂，IC₅₀ 为 0.87 nM。Volasertib 抑制 PLK2 和 PLK3，IC₅₀ 分别为 5 和 56 nM。Volasertib 诱导有丝分裂停滞和细胞凋亡。Volasertib 是一种二氢蝶呤酮衍生物，在多种癌症模型中显示出显着的抗肿瘤活性。

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Volasertib Chemical Structure

CAS No. : 755038-65-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1116	In-stock
1 mg	￥340	In-stock
5 mg	￥820	In-stock
10 mg	￥1300	In-stock
50 mg	￥3750	In-stock
100 mg	￥5200	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Volasertib:

Volasertib trihydrochloride 询价

MCE 顾客使用本产品发表的 24 篇科研文献

Proliferation Assay

: Volasertib purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;43(4):1472-1486. [Abstract]; The addition of Volasertib (0.5-1.5 µg/mL blunts the increase of the percentage of annexin-V-binding erythrocytes following glucose deprivation, an effect reaching statistical significance at 1 and 1.5 µg/mL Volasertib.

Volasertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型

PLK1 PLK2 PLK3 PLK4

生物活性
纯度 & 产品资料
参考文献

生物活性

Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC₅₀s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models^[1]^[2].

IC₅₀ & Target^[3]

PLK1

0.87 nM (IC₅₀)

PLK2

5 nM (IC₅₀)

PLK3

56 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	4137 nM Compound: 3; BI 6727	Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
A-427	IC₅₀	91 nM Compound: 44	Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay	[PMID: 37197456]
A549	IC₅₀	0.08 μM Compound: BI6727; I	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
A549	IC₅₀	206.4 nM Compound: 3; BI 6727	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
DU-145	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HCT-116	IC₅₀	0.11 μM Compound: BI6727; I	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
HCT-116	IC₅₀	602.4 nM Compound: 3; BI 6727	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HEK-293T	IC₅₀	1.1 nM Compound: Volasertib	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
HepG2	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HT-29	IC₅₀	1133 nM Compound: 3; BI 6727	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
JeKo-1	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
K562	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
KARPAS-299	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
L02	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
MCF7	IC₅₀	0.09 μM Compound: BI6727; I	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MDA-MB-231	IC₅₀	0.11 μM Compound: BI6727; I	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MDA-MB-231	IC₅₀	1482 nM Compound: 3; BI 6727	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
MM1.S	IC₅₀	4.5 nM Compound: Volasertib	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
NCI-H23	IC₅₀	53 nM Compound: 44	Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay	[PMID: 37197456]
PC-3	IC₅₀	0.09 μM Compound: BI6727; I	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
SMMC-7721	IC₅₀	77.2 nM Compound: 3; BI 6727	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]

体外研究
(In Vitro)

Volasertib (BI 6727；0.01-10000 nM；72 小时) 在多种细胞系^[1]中的 EC₅₀ 值为 11 至 37 nmol/L。
Volasertib (10-1000 nM；24 小时) 导致细胞积累 4N DNA 含量，表明细胞周期阻滞在 G2-M 期^[1]。
Volasertib (100 nM；24-72 hours) 在 48 小时诱导细胞凋亡^[1]。

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

Cell Proliferation Assay^[1]

Cell Line:	Multiple cell lines
Concentration:	0.01-10000 nM
Incubation Time:	72 hours
Result:	Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC₅₀=23 nmol/L) and lung (NCI-H460, EC₅₀=21 nmol/L), melanoma (BRO, EC₅₀=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC₅₀=15 nmol/L; HL-60, EC₅₀=32 nmol/L; THP-1, E₅₀=36 nmol/L and Raji, EC₅₀=37 nmol/L) with EC₅₀ values of 11 to 37 nmol/L.

Apoptosis Analysis^[1]

Cell Line:	NCI-H460 cells
Concentration:	100 nM
Incubation Time:	24, 48, 72 hours
Result:	G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours.

Cell Cycle Analysis^[1]

Cell Line:	NCI-H460 cells
Concentration:	10, 30, 100, 300, 1000 nM
Incubation Time:	24 hours
Result:	Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.

体内研究
(In Vivo)

Volasertib (BI 6727；每周总剂量为 50 mg/kg；口服；每周一次、每周两次或每天一次；持续 40 天) 在人结肠癌异种移植模型中显示出相当的疗效^[1]。
Volasertib (15、20 或 25 mg/kg/天；静脉注射；每周连续 2 天；持续 40 天) 在人结肠癌异种移植模型中导致显著的肿瘤生长延迟甚至肿瘤消退^[1]。
Volasertib (70 mg/kg，每周一次或每天 10 mg/kg；口服) 显著延迟源自 NCI-H460 细胞的非小细胞肺癌异种移植模型中的肿瘤生长^[1]。
Volasertib (单剂量 40 mg/kg；静脉注射) 导致 HCT 116 荷瘤裸鼠的有丝分裂细胞显著增加 (13 倍)^[1]。
Volasertib 在小鼠体内分布容积大，终末半衰期长 (V_ss=7.6 L/kg，t_1/2=46 h) 和大鼠 (V_ss=22 L/kg，t_1/2=54 h)^[1]。

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

Animal Model:	Female BomTac:NMRI-Foxn1^nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)^[1]
Dosage:	A total weekly dose of 50 mg/kg
Administration:	Oral; once a week, twice a week, or daily; for 40 days
Result:	Showed comparable efficacy and were well tolerated.

Animal Model:	Female BomTac:NMRI-Foxn1^nu mice and male Wistar rats of the strain Crl:WI^[1]
Dosage:	35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis)
Administration:	IV 5-minute infusion; a single dose 5-minute infusion
Result:	Had high volume of distribution and a long terminal half-life in mice (V_ss=7.6 L/kg, t_1/2=46 h) and rats (V_ss=22 L/kg, t_1/2=54 h).

Clinical Trial

分子量

618.81

Formula

C₃₄H₅₀N₈O₃

CAS 号

755038-65-4

性状

固体

颜色

Off-white to light yellow

中文名称

伏拉塞替

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (40.40 mM; 超声助溶 (<60°C); 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	1.6160 mL	8.0800 mL	16.1600 mL
5 mM	0.3232 mL	1.6160 mL	3.2320 mL
10 mM	0.1616 mL	0.8080 mL	1.6160 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

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: ≥ 2.08 mg/mL (3.36 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (3.36 mM); 悬浊液; 超声助溶

此方案可获得 2.08 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 20.8 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: ≥ 2.08 mg/mL (3.36 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.41%

选择批次：

Data Sheet (647 KB) SDS (392 KB)

COA (190 KB) LCMS (100 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Xie FF, et al. Volasertib suppresses tumor growth in cervical cancer. Am J Cancer Res. 2015 Nov 15;5(12):3548-59. [Content Brief]

[2]. Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.Clin Cancer Res. 2009 May 1;15(9):3094-102. Epub [Content Brief]

Volasertib 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	1.6160 mL	8.0800 mL	16.1600 mL	40.4001 mL
	5 mM	0.3232 mL	1.6160 mL	3.2320 mL	8.0800 mL
	10 mM	0.1616 mL	0.8080 mL	1.6160 mL	4.0400 mL
	15 mM	0.1077 mL	0.5387 mL	1.0773 mL	2.6933 mL
	20 mM	0.0808 mL	0.4040 mL	0.8080 mL	2.0200 mL
	25 mM	0.0646 mL	0.3232 mL	0.6464 mL	1.6160 mL
	30 mM	0.0539 mL	0.2693 mL	0.5387 mL	1.3467 mL
	40 mM	0.0404 mL	0.2020 mL	0.4040 mL	1.0100 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.

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Volasertib (Synonyms: 伏拉塞替; BI 6727)

Customer Review

Other Forms of Volasertib:

MCE 顾客使用本产品发表的 24 篇科研文献

Volasertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

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Volasertib 相关分类

完整储备液配制表

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Volasertib (Synonyms: 伏拉塞替; BI 6727)

Customer Review

Other Forms of Volasertib:

Volasertib 相关抗体

MCE 顾客使用本产品发表的 24 篇科研文献

Volasertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Volasertib 相关抗体:

摩尔计算器

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完整储备液配制表

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