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

Volasertib Chemical Structure

CAS: 755038-65-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1654.53 现货
5mg RMB 974.11 现货
25mg RMB 3005.97 现货
100mg RMB 7125.3 现货
1g RMB 13677.3 现货
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客户使用Selleck的Volasertib发表文献160

产品质控

批次: 纯度: 99.78%
99.01

Volasertib相关产品

相关信号通路图

PLK抑制剂选择性比较

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
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
PLK1 [1]
(Cell-free assay)
0.87 nM
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 p-PLK1 / PLK1 p-AKT / AKT / p-MAPK / MAPK PARP / c-myc p-c-Met / c-Met / p-FAK / FAK / p-Src / Src Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3 29108241
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
批次:

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

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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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.

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