- 抑制剂
- 化合物库
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- 生物试剂
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白实验
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag亲和凝胶
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 细胞核与细胞浆蛋白抽提试剂盒
- 免疫磁珠
- 蛋白酶抑制剂Cocktail
- 蛋白酶抑制剂Cocktail(DMSO储液)
- 磷酸酶抑制剂Cocktail
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Volasertib
别名: BI 6727
Volasertib是一种高度有效的Plk1抑制剂，无细胞试验中IC50为0.87 nM，比作用于Plk2和Plk3选择性高6和65倍。Volasertib可在多种癌细胞中诱导细胞周期停滞和自噬。Phase 3。
Volasertib Chemical Structure
CAS: 755038-65-4
产品质控
批次：
纯度：
99.78%
99.78
Volasertib相关产品
| 相关靶点 | PLK1 PLK2 PLK3 PLK4 | 点击展开 |
|---|---|---|
| 相关产品 | BI 2536 Rigosertib (ON-01910) GSK461364 Onvansertib (NMS-P937) SBE 13 HCl HMN-214 Ro3280 CFI-400945 MLN0905 Poloxin | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| DU145 | Growth Inhibition Assay | 10/50/250 nM | 24 h | IC50<10 nM | 23884428 |
| T98G | Growth Inhibition Assay | 50-150 nM | 72 h | inhibits cell proliferation | 23887645 |
| SF188 | Growth Inhibition Assay | 50-150 nM | 72 h | inhibits cell proliferation | 23887645 |
| FaDu | Growth Inhibition Assay | 0-1000 nM | 1-4 d | inhibits cell growth in both dose- and time-dependent manner | 23891096 |
| A431 | Growth Inhibition Assay | 0-30 nM | 1-4 d | inhibits cell growth in both dose- and time-dependent manner | 23891096 |
| HCC1428/LTED | Growth Inhibition Assay | 2.5-40 nM | 5 d | inhibits cell growth in a dose-dependent manner | 25480943 |
| MCF7/LTED | Growth Inhibition Assay | 2.5-40 nM | 5 d | inhibits cell growth in a dose-dependent manner | 25480943 |
| LNCaP | Growth Inhibition Assay | 10/50/250 nM | 24 h | IC50<10 nM | 23884428 |
| PC3 | Growth Inhibition Assay | 10/50/250 nM | 24 h | IC50∼600 nM | 23884428 |
| KMCH-1 | Apoptosis Assay | 200 nM | 24 h | induces apoptosis | 23703673 |
| Mz-ChA-1 | Apoptosis Assay | 200 nM | 24 h | induces apoptosis | 23703673 |
| HUCCT-1 | Apoptosis Assay | 200 nM | 24 h | induces apoptosis | 23703673 |
| THP-1 | Growth Inhibition Assay | 72 h | IC50=56±39 nM | 25576074 | |
| SKM-1 | Growth Inhibition Assay | 72 h | IC50=95±52 nM | 25576074 | |
| OCI-AML3 | Growth Inhibition Assay | 72 h | IC50=90±51 nM | 25576074 | |
| NOMO-1 | Growth Inhibition Assay | 72 h | IC50=145±7 nM | 25576074 | |
| MV-4-11 | Growth Inhibition Assay | 72 h | IC50=16±6 nM | 25576074 | |
| MOLM-13 | Growth Inhibition Assay | 72 h | IC50=57±44 nM | 25576074 | |
| KG-1 | Growth Inhibition Assay | 72 h | IC50=150±67 nM | 25576074 | |
| KASUMI-1 | Growth Inhibition Assay | 72 h | IC50=170±51 nM | 25576074 | |
| RT4 | Growth Inhibition Assay | 48 h | IC50=111.27 nM | 23792639 | |
| 5637 | Growth Inhibition Assay | 48 h | IC50=1165.14 nM | 23792639 | |
| T24 | Growth Inhibition Assay | 48 h | IC50=204.91 nM | 23792639 | |
| SKBR3 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human SKBR3 cells after 24 hrs by MTT assay | 29288948 | |
| MDA-MB-231 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay | 29288948 | |
| MDA-MB-468 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MDA-MB-468 cells after 24 hrs by MTT assay | 29288948 | |
| BT474 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human BT474 cells after 24 hrs by MTT assay | 29288948 | |
| ZR-75-1 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human ZR-75-1 cells after 24 hrs by MTT assay | 29288948 | |
| HCT 116 | Growth Inhibition Assay | EC50 = 23 nM | 19383823 | ||
| NCI-H460 | Growth Inhibition Assay | EC50 = 21 nM | 19383823 | ||
| BRO | Growth Inhibition Assay | EC50 = 11 nM | 19383823 | ||
| GRANTA-519 | Growth Inhibition Assay | EC50 = 15 nM | 19383823 | ||
| HL-60 | Growth Inhibition Assay | EC50 = 32 nM | 19383823 | ||
| THP-1 | Growth Inhibition Assay | EC50 = 36 nM | 19383823 | ||
| Raji | Growth Inhibition Assay | EC50 = 37 nM | 19383823 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Volasertib是一种高度有效的Plk1抑制剂，无细胞试验中IC50为0.87 nM，比作用于Plk2和Plk3选择性高6和65倍。Volasertib可在多种癌细胞中诱导细胞周期停滞和自噬。Phase 3。 | ||
|---|---|---|---|
| 特性 | BI6727具有高的体积分布，良好的组织穿透力和长的半衰期。 | ||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 如同BI2536，BI6727是属于dihydropteridinone类化合物的ATP竞争性激酶抑制剂。除了Plk1，BI6727也有效地抑制两个密切相关的激酶Plk2和Plk3，IC50分别为为5 nM和56 nM。 BI6727在浓度高达10 μM时对五十多种激酶均没有抑制活性。BI6727抑制从各种癌组织来源的多种细胞系的增殖，包括HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1 和 Raji 细胞，EC50 分别为23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM 和 37 nM。在NCI-H460细胞中，BI6727 (100 nM)诱导有丝分裂细胞聚集，这些细胞中有单极纺锤体和组蛋白H3的磷酸丝氨酸10阳性染色，这表明细胞处于M期，随后诱导细胞凋亡。[1] BI6727低纳摩尔浓度表现对神经母细胞瘤（NB）肿瘤起始细胞（NB TIC）的抑制活性，EC 50为21 nM，而只有微摩尔浓度的BI6727对正常小儿神经干细胞有毒性作用。[2] 类似于BI2536，BI6727诱导Daoy和ONS-76髓母细胞瘤细胞的生长停滞。[3] |
|||
|---|---|---|---|---|
| 激酶实验 | 体外激酶抑制试验 | |||
| 重组人类Plk1的（残基1-603）是用杆状病毒表达系统表达的带有NH2末端和GST-标记的融合采用的蛋白质。酶的活性测定法测定Plk1是在梯度稀释的BI6727中进行，以20 ng重组激酶以及10 μg牛乳酪蛋白为底物。激酶反应在60微升的终体积在30℃下进行45分钟[15 mM MgCl2, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi γ-32P-ATP]。反应通过加入125μL冰冷的5％三氯乙酸终止。转移沉淀到多屏幕混合酯纤维素过滤板后，洗涤板用1％三氯乙酸洗涤并测量辐射量。剂量-反应曲线用于计算IC 50值。 | ||||
| 细胞实验 | 细胞系 | HCT116，NCI-H460，BRO，GRANTA-519，HL-60，THP-1，和Raji细胞 | ||
| 浓度 | 溶解在DMSO中至终浓度约1 μM | |||
| 孵育时间 | 24, 48和72小时 | |||
| 方法 | 细胞增殖测定是将细胞孵育在不同浓度的BI6727中24，48和72小时，而后在荧光分光光度计上通过测量的Alamar蓝染料的转换测定。有效浓度在哪些细胞生长是由50％（EC 50）抑制从剂量 - 反应曲线拟合推断的。为了确定DNA含量，细胞悬浮液被固定在80％乙醇中，用含0.25％Triton X-100的PBS处理5分钟，并用含0.1％RNA酶和10 μg/mL的碘化丙锭的PBS室温孵育20分钟。细胞周期的测定是用流式细胞仪分析的。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3 p-c-Met / c-Met / p-FAK / FAK / p-Src / Src PARP / c-myc p-AKT / AKT / p-MAPK / MAPK p-PLK1 / PLK1 |
|
31040125 | |
| Immunofluorescence | PLK1 / Wee1 |
|
29108241 | |
| Growth inhibition assay | Cell viability |
|
29383095 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | BI6727显著抑制多种人类肿瘤异种移植物的生长，包括HCT116, NCI-H460, 和紫杉类耐药CXB1结肠癌，伴随着增加的有丝分裂指数以及细胞凋亡的增加。[1] 体内研究表明，BI6727表现出比BI2536更好的毒性和药动学特征。[3] |
|
|---|---|---|
| 动物实验 | Animal Models | 雌性BomTac：NMRI-Foxn1 NU小鼠腹腔移植HCT116，NCI-H460，或CXB1细胞。 |
| Dosages | 约25 mg/kg/day | |
| Administration | 静脉注射，或通过灌胃针 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02722135 | Withdrawn | Leukemia Myeloid Acute |
Boehringer Ingelheim |
November 2016 | Phase 1 |
| NCT02721875 | Terminated | Myelodysplastic Syndromes |
Boehringer Ingelheim |
April 28 2016 | Phase 1 |
| NCT02201329 | Completed | Myelodysplastic Syndromes|Leukemia Myelomonocytic Chronic |
Boehringer Ingelheim |
August 2014 | Phase 1 |
| NCT01971476 | Completed | Leukemia|Neoplasms |
Boehringer Ingelheim |
October 22 2013 | Phase 1 |
| NCT01772563 | Completed | Neoplasms |
Boehringer Ingelheim |
February 4 2013 | Phase 1 |
| NCT01662505 | Completed | Leukemia Myeloid Acute |
Boehringer Ingelheim |
August 2012 | Phase 1 |
|
化学信息&溶解度
| 分子量 | 618.81 | 分子式 | C34H50N8O3 |
| CAS号 | 755038-65-4 | SDF | Download Volasertib SDF |
| Smiles | CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 35 mg/mL ( (56.56 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
I wonder how to reconstitute the inhibitor for in vivo studies?
回答：
Volasertib can be dissolved in 4% DMSO+Corn oil at 2mg/ml for i.p. injection in mice. For oral administration, it can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose as indicated in the publications. We also suggest the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol for a suspension which we tested in house.
