Volasertib (BI 6727)

目录号:S2235

Volasertib (BI 6727) Chemical Structure

Molecular Weight(MW): 618.81

Volasertib (BI 6727)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。Phase 3。

规格 价格 库存 购买数量  
In DMSO RMB 1654.53 现货
RMB 974.11 现货
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产品安全说明书

PLK抑制剂选择性比较

生物活性

产品描述 Volasertib (BI 6727)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。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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KASUMI-1 NVzWeItKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GxXFczKGh? MYjJR|UxRTF5MNMxOVEhdk1? NIPWOWszPTV5NkC3OC=>
KG-1 Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LTclczKGh? MXrJR|UxRTF3MNMxOlchdk1? NHv5UXkzPTV5NkC3OC=>
MOLM-13 MojYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmL2O|IhcA>? M3XkbGlEPTB;NUhCtVQ1KG6P MVSyOVU4PjB5NB?=
MV-4-11 NWPJRpBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGeycVI4OiCq MXLJR|UxRTF4wsG2JI5O M4P5bFI2PTd4MEe0
NOMO-1 M1XOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHUdnc5PzJiaB?= NXfHd5JuUUN3ME2xOFXDuTdibl2= M{HRR|I2PTd4MEe0
OCI-AML3 M4TZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4G3ZVczKGh? NEPucnNKSzVyPUmwxtE2OSCwTR?= NFfWUoszPTV5NkC3OC=>
SKM-1 NGPXWY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHj2WHM4OiCq NEPlOlRKSzVyPUm1xtE2OiCwTR?= NYC4XJNxOjV3N{[wO|Q>
THP-1 NIT5fHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[4W|E2PzJiaB?= MWnJR|UxRTV4wsGzPUBvVQ>? MmLDNlU2PzZyN{S=
MCF7/LTED  NWDVdYo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOyMlUuPDBibl2= MoTnOUBl M2roV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXGyOVQ5ODl2Mx?=
HCC1428/LTED M4nFTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkD5Nk42NTRyIH7N MmjhOUBl M2Pj[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NU\OOXVYOjV2OEC5OFM>
A431 MkLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPjNE0{OCCwTR?= MVexMVQh\A>? NFTPZoNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NX\ZcnZrOjN6OUGwPVY>
FaDu  NIrhTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnleGsxNTFyMECgcm0> M{[3OVEuPCCm NWXPZ28{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U1l\XCnbnTlcpQhdWGwbnXy NFjCWJozOzh7MUC5Oi=>
SF188 M1LNNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUW1NE0yPTBibl2= NY\aTmgzPzJiaB?= M4\ObmROW09? MnzEbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u Mnj0NlM5QDd4NEW=
T98G MlnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[1NE0yPTBibl2= M1ftdlczKGh? NYj1UJMzTE2VTx?= NIrEV49qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M3fvSVI{QDh5NkS1
DU145 NIHvdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO4NGwyOC93MD:yOVAhdk1? MkK4NlQhcA>? M1XpdmlEPTB:MUCgcm0> NVLYWJloOjN6OES0Nlg>
LNCaP MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\4XlhsOTBxNUCvNlUxKG6P MV6yOEBp NXjBTphRUUN3MEyxNEBvVQ>? MljvNlM5QDR2Mki=
PC3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLJWGoyOC93MD:yOVAhdk1? M1Lt[VI1KGh? MV7JR|Ux6oj:NkCwJI5O NF2xNmYzOzh6NESyPC=>
RT4 NXnHV4tXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[4OFghcA>? MnnWTWM2OD1zMUGuNlchdk1? M1TLWVI{Pzl{NkO5
5637 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:zdnh7PDhiaB?= NX3leGd5UUN3ME2xNVY2NjF2IH7N Ml7UNlM4QTJ4M{m=
T24 NGfHV49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPXOFghcA>? MWPJR|UxRTJyND65NUBvVQ>? M2\JSFI{Pzl{NkO5
KMCH-1 NWjYNnJRSXCxcITvd4l{KEG|c3H5 M3WzfVIxOCCwTR?= MnX5NlQhcA>? NUf5PWtkcW6mdXPld{BieG:ydH;zbZM> MlnJNlM4ODN4N{O=
Mz-ChA-1 MVLBdI9xfG:|aYOgRZN{[Xl? Mkj2NlAxKG6P NGnhc|EzPCCq NWLafJRFcW6mdXPld{BieG:ydH;zbZM> MVKyN|cxOzZ5Mx?=
HUCCT-1 M2DsOmFxd3C2b4Ppd{BCe3OjeR?= M2\tb|IxOCCwTR?= NF;Mb2wzPCCq MkDObY5lfWOnczDhdI9xfG:|aYO= NV\0cHFYOjN5MEO2O|M>
HCT 116 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvDSWM2OMLiPTCyN{BvVQ>? M2\DWVE6Ozh|OEKz
NCI-H460 M4XrfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTFR|UxyqB;IEKxJI5O MUKxPVM5Ozh{Mx?=
BRO MmnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nP[GVEPTEEoE2gNVEhdk1? M1PsUlE6Ozh|OEKz
GRANTA-519 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDuSWM2OMLiPTCxOUBvVQ>? MmXyNVk{QDN6MkO=
HL-60 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPWSWM2OMLiPTCzNkBvVQ>? MWexPVM5Ozh{Mx?=
THP-1 NIPFNZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T3OWVEPTBiPTCzOkBvVQ>? NYnVeWdVOTl|OEO4NlM>
Raji M1TsPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Lne2VEPTBiPTCzO{BvVQ>? NWnyNJpzOTl|OEO4NlM>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-PLK1 / PLK1; 

PubMed: 29108241     


The protein expression of PLK1 and its phosphorylation levels at 24 hours after volasertib treatment in HL-60 and K562 cells.

p-AKT / AKT / p-MAPK / MAPK; 

PubMed: 29108241     


Phosphorylation levels of AKT and MAPK in AML cell lines after volasertib administration.

PARP / c-myc; 

PubMed: 29383095     


Treatment with volasertib (24 hours) induces PARP cleavage and decreases total c-myc expression in the indicated lymphoma cell lines. From left to right: diffuse large B-cell lymphomas (DLBCL), anaplastic large cell lymphoma (ALCL), cutaneous T-cell lymphoma (CTCL) and, peripheral T-cell lymphomas non-otherwise specified (PTCL-NOS). Protein expression was evaluated by immunoblotting.

p-c-Met / c-Met / p-FAK / FAK / p-Src / Src ; 

PubMed: 31040125     


The same cell lines treated identically were subjected to immunoblotting for the indicated proteins (upper) with densitometric quantification normalized with b-actin (lower).

Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3; 

PubMed: 31040125     


Epithelial and mesenchymal non-small-cell lung cancer (NSCLC) cell lines after treatment with 50 nM volasertib for 24 h. Cells were then harvested, and lysates were immunoblotted for the indicated proteins.

29108241 29383095 31040125
Immunofluorescence
PLK1 / Wee1; 

PubMed: 29108241     


The protein expressions of PLK1 and Wee1 were evaluated by immunofluorescent staining. Both parental and volasertib-resistant MOLM14 and HL-60 cells were treated with 50 nM volasertib for 18 hours.

29108241
Growth inhibition assay
Cell viability; 

PubMed: 29383095     


Survival of different B-cell and T-cell lymphoma cell lines upon treatment with indicated doses of Volasertib at 72 hrs. 

29383095
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

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:[1]
+ 展开
  • Cell lines: HCT116,NCI-H460,BRO,GRANTA-519,HL-60,THP-1,和Raji细胞
  • Concentrations: 溶解在DMSO中至终浓度约1 μM
  • Incubation Time: 24, 48和72小时
  • Method: 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。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 雌性BomTac:NMRI-Foxn1 NU小鼠腹腔移植HCT116,NCI-H460,或CXB1细胞。
  • Formulation: 配制成盐酸(0.1N),并用0.9%的NaCl稀释,或悬浮在0.5%的Natrosol250羟乙基纤维素。
  • Dosages: 约25 mg/kg/day
  • Administration: 静脉注射,或通过灌胃针
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 20 mg/mL warmed (32.32 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+corn oil
2mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 618.81
化学式

C34H50N8O3

CAS号 755038-65-4
储存条件 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02757248 Withdrawn PTCL|CTCL Anne Beaven MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University November 2016 Phase 1
NCT02722135 Withdrawn Leukemia Myeloid Acute Boehringer Ingelheim November 2016 Phase 1
NCT02527174 Withdrawn Leukemia Myeloid Acute|Leukemia Monocytic Acute|Leukemia Myelomonocytic Acute|Leukemia Erythroblastic Acute|Leukemia Megakaryoblastic Acute University of Alberta November 2016 Phase 1
NCT02757248 Withdrawn PTCL|CTCL Anne Beaven MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University November 2016 Phase 1
NCT02722135 Withdrawn Leukemia Myeloid Acute Boehringer Ingelheim November 2016 Phase 1
NCT02527174 Withdrawn Leukemia Myeloid Acute|Leukemia Monocytic Acute|Leukemia Myelomonocytic Acute|Leukemia Erythroblastic Acute|Leukemia Megakaryoblastic Acute University of Alberta November 2016 Phase 1

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操作手册

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID