ホームページ Cell Cycle PLK inhibitor - Apoptosis related activator Volasertib For research use only.

Volasertib

別名：BI 6727

Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.

Volasertib化学構造

CAS No. 755038-65-4

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 37000 国内在庫あり
JPY 29500 国内在庫あり
JPY 71500 国内在庫あり
JPY 145500 国内在庫あり
JPY 295500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例（169）

製品安全説明書

現在のバッチを見る： 純度： 99.78%
99.78

Volasertib関連製品

シグナル伝達経路

PLK Signaling Pathways

PLKシグナル伝達経路

PLK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.
特性 A high volume of distribution, indicating good tissue penetration, and a long terminal half-life.
Targets
PLK1 [1]
(Cell-free assay)
0.87 nM
In Vitro
In vitro

Like BI2536, BI6727 is an ATP-competitive kinase inhibitor from the dihydropteridinone class of compounds. In addition to Plk1, BI6727 also potently inhibits two closely related kinases Plk2 and Plk3 with IC50 of 5 nM and 56 nM, respectively. BI6727 at concentrations up to 10 μM displays no inhibitory activity against a panel of >50 other kinases. BI6727 inhibits the proliferation of multiple cell lines derived from various cancer tissues, including HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji cells with EC50 of 23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM, and 37 nM, respectively. BI6727 treatment (100 nM) in NCI-H460 cells induces an accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10, confirming that cells are arrested early in the M phase, followed by induction of apoptosis. [1] Low nanomolar concentrations of BI6727 display potent inhibitory activity against neuroblastoma (NB) tumor-initiating cells (NB TIC) with EC50 of 21 nM, whereas only micromolar concentrations of BI6727 are cytotoxic for normal pediatric neural stem cells. [2] BI6727 induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536. [3]
Kinase Assay In vitro kinase assays
Recombinant human Plk1 (residues 1-603) is expressed as NH2-terminal, GST-tagged fusion protein using a baculoviral expression system and purified by affinity chromatography using glutathione-agarose. Enzyme activity assays for Plk1 are done in the presence of serially diluted BI6727 using 20 ng of recombinant kinase and 10 μg casein from bovine milk as substrate. Kinase reactions are done in a final volume of 60 μL for 45 minutes at 30 °C [15 mM MgCl2, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi γ-32P-ATP]. Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transferring the precipitates to MultiScreen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curves are used for calculating IC50 value.
細胞実験 細胞株 HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji
濃度 Dissolved in DMSO, final concentrations ~1 μM
反応時間 24, 48, and 72 hours
実験の流れ

Cell proliferation assays are done by incubating cells in the presence of various concentrations of BI6727 for 24, 48, and 72 hours and cell growth is assessed by measuring Alamar blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth is inhibited by 50% (EC50) are extrapolated from the dose-response curve fit. To determine the DNA content, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide in PBS for 20 minutes at room temperature. Cell cycle profiles are determined by flow cytometric analysis.
実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo

Administration of BI6727 significantly inhibits the growth of multiple human carcinoma xenografts including HCT116, NCI-H460, and taxane-resistant CXB1 colon carcinoma, accompanied by an increase in the mitotic index as well as an increase in apoptosis. [1] In in vivo studies, BI6727 shows better toxicity and pharmacokinetic profile compared to BI2536. [3]
動物実験 動物モデル Female BomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
投与量 ~25 mg/kg/day
投与経路 Injected i.v., or given intragastrally via gavage needle
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

化学情報

分子量 618.81 化学式

C34H50N8O3
CAS No. 755038-65-4 SDF Download Volasertib SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 35 mg/mL ( (56.56 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問（FAQ）

質問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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