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首页 / 抑制剂/激动剂 / 细胞周期 / PLK / Volasertib/伏拉塞替

Volasertib/伏拉塞替 {[allProObj[0].p_purity_real_show]}

货号：A232139 同义名： BI 6727

Volasertib（BI 6727）是一种口服活性、高效和ATP竞争性的Polo样激酶1（PLK1）抑制剂，IC50为0.87 nM。它抑制PLK2和PLK3，IC50值分别为5 nM和56 nM，诱导有丝分裂停滞和凋亡。Volasertib是一种二氢蝶啶酮衍生物，在多种癌症模型中表现出显著的抗肿瘤活性。

Volasertib/伏拉塞替 化学结构 CAS号：755038-65-4
Volasertib/伏拉塞替 化学结构
CAS号：755038-65-4
Volasertib/伏拉塞替 3D分子结构
CAS号：755038-65-4
Volasertib/伏拉塞替 化学结构 CAS号：755038-65-4
Volasertib/伏拉塞替 3D分子结构 CAS号：755038-65-4
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Volasertib/伏拉塞替 纯度/质量文件 产品仅供科研

货号：A232139 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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产品名称 PLK1 ↓ PLK2 ↓ PLK3 ↓ PLK4 ↓ 其他靶点 纯度
HMN-214 ✔ 99%+
SBE13 HCl ++++

PLK1, IC50: 200 pM

 		98%
Onvansertib +++

PLK1, IC50: 2 nM

 		99%+
Volasertib ++++

PLK1, IC50: 0.87 nM

 		97%
GSK461364 +++

PLK1, Ki: 2.2 nM

 		99%+
MLN0905 +++

PLK1, IC50: 2 nM

 		99%+
Ro3280 ++

PLK1, IC50: 3 nM

 		99%
(E/Z)-Rigosertib sodium +

PLK1, IC50: 9 nM

 		+

PLK2, IC50: 260 nM

 		Bcr-Abl 99%+
BI 2536 ++++

PLK1, IC50: 0.83 nM

 		++

PLK2, IC50: 3.5 nM

 		+

PLK3, IC50: 9.0 nM

 		99%+
CFI-400945 ++

PLK4, IC50: 2.8 nM

 		Tie-2 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Volasertib/伏拉塞替 生物活性

靶点

  • PLK1

    PLK1, IC50:0.87 nM
描述 BI 6727 is a highly potent PLK inhibitor with IC50 values of 0.87nM, 5nM and 56nM for PLK1, 2 and 3, respectively. Volasertib inhibited proliferation of multiple cell lines with EC50 values of 23nM, 21nM, 11nM, 15nM, 32nM, 36nM and 37nM for HCT 116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1 and Raji cell line, respectively. BI 6727 induced apoptosis, shown by cleaved PARP, in NCI-H460 cells at 100nM post 24h and 48h. An accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10 of NCI-H460 cells could also be observed post BI 6727 treatment, confirming that cells are arrested early in the M phase. It exhibited marked antitumor activity in multiple cancer models, including models xenograft HCT 116, NCI-H460 and CXB1 15 cells as well as a model of taxane-resistant colorectal cancer, with oral and i.v. routes of administration at doses ranging in 7-70mg/kg.
作用机制 BI 6727 binds in the ATP binding pocket of Plk1.[1]

Volasertib/伏拉塞替 细胞实验

Cell Line
Concentration Treated Time Description References
HMC-1.1 and HMC-1.2 cells 500 nM 24 h To evaluate the effects of Volasertib on the clonogenic potential and apoptosis of HMC-1 cells, results showed that Volasertib significantly reduced clonogenic growth and induced apoptosis in HMC-1 cells. Biomark Res. 2023 Mar 10;11(1):29.
HGSOC cells 0.001–10 µM 72 h To evaluate the cytotoxicity of Volasertib on HGSOC spheroids and organoids Cells. 2025 Jan 17;14(2):133.
HNSCC cell lines 0.018 to 9.613 μM 72 h To evaluate the sensitivity of HNSCC cell lines to Volasertib, results showed diverse sensitivity among the cell lines Cancer Lett. 2017 Apr 28;392:71-82.
HNSCC cell lines 50 nM To assess the effect of Volasertib on cell cycle and apoptosis in HNSCC cell lines, results showed drug-induced G2/M cell cycle arrest and apoptosis Cancer Lett. 2017 Apr 28;392:71-82.
H1975 50 nM 72 h Induction of a mesenchymal phenotype significantly increased PARP cleavage and DNA damage after Volasertib treatment, indicating enhanced apoptosis. EMBO Mol Med. 2019 May;11(5):e9960.
HCC4006 50 nM 72 h Induction of a mesenchymal phenotype significantly increased PARP cleavage and DNA damage after Volasertib treatment, indicating enhanced apoptosis. EMBO Mol Med. 2019 May;11(5):e9960.
HCC366 50 nM 72 h Induction of a mesenchymal phenotype significantly increased PARP cleavage and DNA damage after Volasertib treatment, indicating enhanced apoptosis. EMBO Mol Med. 2019 May;11(5):e9960.
MIA PaCa-2-R 20 nM 24 h To evaluate the sensitivity of Volasertib in KRASG12Ci-resistant cells, results showed that Volasertib significantly reduced c-Myc levels and induced apoptosis. Exp Hematol Oncol. 2023 Dec 16;12(1):105.
NCI-H358-R 20 nM 24 h To evaluate the sensitivity of Volasertib in KRASG12Ci-resistant cells, results showed that Volasertib significantly reduced c-Myc levels and induced apoptosis. Exp Hematol Oncol. 2023 Dec 16;12(1):105.
SW1573 20 nM 24 h To evaluate the sensitivity of Volasertib in KRASG12Ci-resistant cells, results showed that Volasertib significantly reduced c-Myc levels and induced apoptosis. Exp Hematol Oncol. 2023 Dec 16;12(1):105.
K562-S cells 1 μM 24 h To evaluate the effect of Volasertib on the expression and activation of AURKA, PLK1, and FOXM1 in K562-S cells. The results showed that Volasertib significantly reduced the expression and activation of AURKA, PLK1, and FOXM1. J Exp Clin Cancer Res. 2019 May 23;38(1):216.
K562-R cells 1 μM 24 h To evaluate the effect of Volasertib on the expression and activation of AURKA, PLK1, and FOXM1 in K562-R cells. The results showed that Volasertib significantly reduced the expression and activation of AURKA, PLK1, and FOXM1. J Exp Clin Cancer Res. 2019 May 23;38(1):216.

Volasertib/伏拉塞替 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice AA TNBC xenograft model Intraperitoneal injection 15 mg/kg Twice weekly for 28 days To evaluate the effect of Volasertib on the growth of AA TNBC xenograft tumors, the results showed that Volasertib significantly inhibited the growth of AA TNBC tumors. Cell Death Dis. 2023 Jan 10;14(1):12
Mice Oral squamous tongue tumor model Intravenous injection 30 mg/kg Weekly for 21 days To evaluate the antitumor effect of Volasertib in an AJUBA-mutant HNSCC mouse model, results showed significant reduction in tumor volume Cancer Lett. 2017 Apr 28;392:71-82.
Mice NSCLC cell line and patient-derived xenograft (PDX) models Intravenous 30 mg/kg Weekly for 5 weeks Volasertib alone significantly reduced tumor growth in mesenchymal models but was less effective in epithelial models. The combination of Volasertib and cMet inhibitors led to significant tumor regression. EMBO Mol Med. 2019 May;11(5):e9960.
Nude mice KRASG12C-mutant tumor models Oral 20 mg/kg Once per week for 3–4 weeks To evaluate the inhibitory effect of Volasertib combined with KRASG12Ci on KRASG12C-mutant tumors, results showed that the combination therapy significantly inhibited tumor growth and overcame drug resistance. Exp Hematol Oncol. 2023 Dec 16;12(1):105.
Mice NSG mice Intraperitoneal injection 5 mg/kg Every other day, up to 20 injections To evaluate the therapeutic effect of Volasertib in combination with Venetoclax on T-ALL mouse models, the results showed that the combination treatment significantly reduced tumor burden and improved the survival rate of the mice. Blood Cancer J. 2023 Sep 7;13(1):139

Volasertib/伏拉塞替 动物研究

Dose Mice: 30 mg/kg[2] (i.v.), 40 mg/kg[1] (i.v.), 50 mg/kg[1] (p.o.) Rat: 10 mg/kg[1] (i.v.), 30 mg/kg[1] (p.o.)
Administration i.v., p.o.
Pharmacokinetics
Animal Mice[1] Rats[1]
Dose 35 mg/kg (i.v.)
50 mg/kg (p.o.) 		10 mg/kg (i.v.)
30 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o.
F 41% (p.o.) 55% (p.o.)
AUC0→inf 100 µmol·h/l (i.v.)
T1/2 46 h (i.v.) 54 h (i.v.)
Tmax 1.7 h (p.o.) 6.7 h (p.o.)
AUC0-inf 30 µmol·h/l (i.v.)
CL 10 ml/min/kg (i.v.) 8.9 ml/min/kg (i.v.)
Cmax 7.1 µmol/l (i.v.)
5.7 µmol/l (p.o.) 		11.9 µmol/l (i.v.)
2.2 µmol/l (p.o.)
Vss 7.6 L/kg (i.v.) 22 L/kg (i.v.)
AUC0→24h 58 µmol·h/l (p.o.) 34 µmol·h/l (p.o.)

Volasertib/伏拉塞替 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01023958 Neoplasms Phase 2 Completed - United States, California ... 展开 >> 1230.2.5 Boehringer Ingelheim Investigational Site Beverly Hills, California, United States 1230.2.10 Boehringer Ingelheim Investigational Site Los Angeles, California, United States United States, Florida 1230.2.34 Boehringer Ingelheim Investigational Site Miami, Florida, United States 1230.2.29 Boehringer Ingelheim Investigational Site Orlando, Florida, United States United States, Illinois 1230.2.6 Boehringer Ingelheim Investigational Site Chicago, Illinois, United States 1230.2.17 Boehringer Ingelheim Investigational Site Joliet, Illinois, United States United States, Louisiana 1230.2.24 Boehringer Ingelheim Investigational Site Metairie, Louisiana, United States United States, Maryland 1230.2.1 Boehringer Ingelheim Investigational Site Baltimore, Maryland, United States United States, Nevada 1230.2.25 Boehringer Ingelheim Investigational Site Las Vegas, Nevada, United States 1230.2.36 Boehringer Ingelheim Investigational Site Las Vegas, Nevada, United States United States, New Hampshire 1230.2.19 Boehringer Ingelheim Investigational Site Lebanon, New Hampshire, United States United States, New York 1230.2.20 Boehringer Ingelheim Investigational Site New York, New York, United States 1230.2.23 Boehringer Ingelheim Investigational Site New York, New York, United States United States, North Carolina 1230.2.12 Boehringer Ingelheim Investigational Site Charlotte, North Carolina, United States United States, Pennsylvania 1230.2.4 Boehringer Ingelheim Investigational Site Philadelphia, Pennsylvania, United States United States, Texas 1230.2.38 Boehringer Ingelheim Investigational Site Beaumont, Texas, United States 1230.2.41 Boehringer Ingelheim Investigational Site Tyler, Texas, United States 1230.2.43 Boehringer Ingelheim Investigational Site Webster, Texas, United States United States, Virginia 1230.2.44 Boehringer Ingelheim Investigational Site Fairfax, Virginia, United States Taiwan 1230.2.51 Boehringer Ingelheim Investigational Site Tainan, Taiwan 1230.2.50 Boehringer Ingelheim Investigational Site Taipei, Taiwan 收起 <<
NCT00969553 Neoplasms Phase 1 Completed - Taiwan ... 展开 >> 1230.16.886002 Boehringer Ingelheim Investigational Site Tainan, Taiwan 1230.16.886001 Boehringer Ingelheim Investigational Site Taipei, Taiwan 收起 <<
NCT01023958 - Completed - -

Volasertib/伏拉塞替 参考文献

[1]Rudolph D, Steegmaier M, 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.

[2]Gorlick R, Kolb EA, et al. Initial testing (stage 1) of the Polo-like kinase inhibitor volasertib (BI 6727), by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2014 Jan;61(1):158-64.

Volasertib/伏拉塞替 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.08mL

1.62mL

0.81mL

16.16mL

3.23mL

1.62mL

Volasertib/伏拉塞替 技术信息

CAS号755038-65-4
分子式C34H50N8O3
分子量 618.81
SMILES Code O=C(C1=CC=C(C(OC)=C1)NC2=NC3=C(C=N2)N(C([C@H](N3C(C)C)CC)=O)C)N[C@H]4CC[C@@H](CC4)N5CCN(CC5)CC6CC6
MDL No. MFCD20926414
别名 BI 6727
运输蓝冰
InChI Key SXNJFOWDRLKDSF-XKHVUIRMSA-N
Pubchem ID 10461508
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(80.8 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 二
方案 三

Tags: Volasertib | BI 6727 | PLK | AmBeed-信号通路专用抑制剂 | Volasertib/伏拉塞替 纯度/质量文件 | Volasertib/伏拉塞替 亚型比较 | Volasertib/伏拉塞替 生物活性 | Volasertib/伏拉塞替 动物研究 | Volasertib/伏拉塞替 临床数据 | Volasertib/伏拉塞替 参考文献 | Volasertib/伏拉塞替 实验方案 | Volasertib/伏拉塞替 技术信息

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