Volasertib (BI 6727)

製品コードS2235

Volasertib (BI 6727)化学構造

分子量(MW):618.81

Volasertib (BI 6727)は一種の高度有効なPlk1阻害剤で、無細胞試験でこのIC50値が0.87nMですが、Plk1に作用する選択性はPlk2とPlk3に作用する選択性より6倍と65倍がそれぞれ高くなります。臨床3期。

サイズ 価格(税別) 在庫  
JPY 33532.00 あり
JPY 19920.00 あり

カスタマーフィードバック(5)

  • Western blot analysis. HeLa or MCF7 cells were treated with nocodazole (noc, 50 ng/ml), paclitaxel (pacli, 50 nM), the Plk1 inhibitor BI 2536 (50 nM) or BI 6727 (50 nM) for 16 h and cellular extracts were prepared for western blot analysis with antibodies as indicated. con: cellular extracts from control cells without any treatment. β-actin served as loading control.

    Oncogene 2013 10.1038/onc.2013.518. Volasertib (BI 6727) purchased from Selleck.

    immunoblot analyses were performed in A375 xenografted melanoma tissues treated with BI 6727 (10 and 25 mg/kg body weight) or vehicle alone to determine the effect of PLK1 knockdown using (D) PCK1 and (E) FBP1 antibodies. The blots were re-probed with b-actin for loading control. Data is representative of three individual experiments. (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article)

    Cancer Lett, 2017, 394:13-21. Volasertib (BI 6727) purchased from Selleck.

  • HNSCC cell-cycle stages determined according to 7-aminoactinomycin D and BrdU incorporation.

    Cancer Lett, 2017, 392:71-82. Volasertib (BI 6727) purchased from Selleck.

    Decrease viability of Hec50 subclones after 3 days treatment with BI6727 was shown. Reduction of Cdc2 Tyr15 phosphorylation and increase Histone H3 Ser10 phosphorylation in cells treated with BI 6727 was observed.

    Dr. Xiangbing Meng from University of Iowa. Volasertib (BI 6727) purchased from Selleck.

  • Hec50 cells are arrested in mitosis after 24hours treatment with 10nM BI 6727.

    Dr. Xiangbing Meng from University of Iowa. Volasertib (BI 6727) purchased from Selleck.

製品安全説明書

PLK阻害剤の選択性比較

生物活性

製品説明 Volasertib (BI 6727)は一種の高度有効なPlk1阻害剤で、無細胞試験でこのIC50値が0.87nMですが、Plk1に作用する選択性はPlk2とPlk3に作用する選択性より6倍と65倍がそれぞれ高くなります。臨床3期。
特性 A high volume of distribution, indicating good tissue penetration, and a long terminal half-life.
ターゲット
PLK1 [1]
(Cell-free assay)
0.87 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KASUMI-1 M{\hdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHroSYk4OiCq NELy[21KSzVyPUG3NOKyPTFibl2= M4nLVlI2PTd4MEe0
KG-1 NV\kOJZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVq3NkBp M3vR[2lEPTB;MUWwxtE3PyCwTR?= NGHHTmIzPTV5NkC3OC=>
MOLM-13 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG3NkBp NVLNWGpVUUN3ME21O:KyPDRibl2= NYXt[pRPOjV3N{[wO|Q>
MV-4-11 M4LTTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7DeVJKPzJiaB?= MXrJR|UxRTF4wsG2JI5O NFPzcXczPTV5NkC3OC=>
NOMO-1 MojYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDMfmY4OiCq NEnIO4xKSzVyPUG0OeKyPyCwTR?= M13CXFI2PTd4MEe0
OCI-AML3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HCclczKGh? NEfXdFVKSzVyPUmwxtE2OSCwTR?= M2nic|I2PTd4MEe0
SKM-1 NWL0ToE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXW3NkBp NVTOZohGUUN3ME25OeKyPTJibl2= MmL0NlU2PzZyN{S=
THP-1 MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO3NkBp MWjJR|UxRTV4wsGzPUBvVQ>? NIjRVnozPTV5NkC3OC=>
MCF7/LTED  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu5Nk42NTRyIH7N NILUT2k2KGR? MV3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NITxOnAzPTR6MEm0Ny=>
HCC1428/LTED NGfmTnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXiyMlUuPDBibl2= MVm1JIQ> Mkm2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEjaU3ozPTR6MEm0Ny=>
A431 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjjPVBXOC1|MDDuUS=> NXnuenRsOS12IHS= MYnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? M2fH[VI{QDlzMEm2
FaDu  NF:xdYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnEW3ExNTFyMECgcm0> MknjNU01KGR? NELLcWpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NF6wWYUzOzh7MUC5Oi=>
SF188 M2S0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXPR|E2OC1zNUCgcm0> M4nQ[lczKGh? MYjEUXNQ MXLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MV:yN|g5PzZ2NR?=
T98G MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYq1NE0yPTBibl2= M2fZd|czKGh? NH7XXYtFVVOR MlzvbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NV6yfmFSOjN6OEe2OFU>
DU145 MnPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLUcG4{OTBxNUCvNlUxKG6P NWXsPZFrOjRiaB?= MYfJR|UxRDFyIH7N NFz4UlYzOzh6NESyPC=>
LNCaP MnywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXixNE82OC9{NUCgcm0> MUOyOEBp NFThR3ZKSzVyPEGwJI5O NIrr[FczOzh6NESyPC=>
PC3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjnfW9NOTBxNUCvNlUxKG6P NIPjV3kzPCCq MWPJR|Ux6oj:NkCwJI5O NG\uWpEzOzh6NESyPC=>
RT4 NIq2cmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEG0XpE1QCCq M{OzVGlEPTB;MUGxMlI4KG6P NHP4eHczOzd7Mk[zPS=>
5637 NF\mbJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVK0PEBp M4fkeWlEPTB;MUG2OU4yPCCwTR?= MkfZNlM4QTJ4M{m=
T24 NELScZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPoN4k1QCCq MV;JR|UxRTJyND65NUBvVQ>? M1e1VlI{Pzl{NkO5
KMCH-1 M4jsR2Fxd3C2b4Ppd{BCe3OjeR?= M2XtS|IxOCCwTR?= NVrOe48yOjRiaB?= MYfpcoR2[2W|IHHwc5B1d3Orcx?= NXu0W4RiOjN5MEO2O|M>
Mz-ChA-1 NGWwXYFCeG:ydH;zbZMhSXO|YYm= NVXuR2RmOjByIH7N NInPd2czPCCq NUPURXBqcW6mdXPld{BieG:ydH;zbZM> NEnKW2szOzdyM{[3Ny=>
HUCCT-1 M{HZdGFxd3C2b4Ppd{BCe3OjeR?= M3LEc|IxOCCwTR?= M3:zWFI1KGh? NGjOVlhqdmS3Y3XzJIFxd3C2b4Ppdy=> NEHwZ|MzOzdyM{[3Ny=>
HCT 116 NILWb|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLYSJo4TUN3MNMgQUAzOyCwTR?= MmXUNVk{QDN6MkO=
NCI-H460 M3Pwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInOWYlGSzVywrC9JFIyKG6P NIfE[JgyQTN6M{iyNy=>
BRO MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6yUHpnTUN3MNMgQUAyOSCwTR?= NIHTU2UyQTN6M{iyNy=>
GRANTA-519 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Tuc2VEPTEEoE2gNVUhdk1? MkGwNVk{QDN6MkO=
HL-60 NE\DUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;SUWxVTUN3MNMgQUA{OiCwTR?= NE\xb28yQTN6M{iyNy=>
THP-1 NXv3Wnd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\FR|UxKD1iM{[gcm0> M2HlO|E6Ozh|OEKz
Raji NF\rVopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\6PFgyTUN3MDC9JFM4KG6P MlTsNVk{QDN6MkO=

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Female BomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
  • 製剤: Formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose
  • 投薬量: ~25 mg/kg/day
  • 投与方法: Injected i.v., or given intragastrally via gavage needle
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 20 mg/mL (32.32 mM) warming
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+corn oil
2mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 618.81
化学式

C34H50N8O3

CAS No. 755038-65-4
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02722135 Withdrawn Leukemia, Myeloid, Acute Boehringer Ingelheim November 2016 Phase 1
NCT02527174 Not yet recruiting 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
NCT02875002 Not yet recruiting Relapsed and Refractory Aggressive B- and T-cell Lymphomas|Lymphoma Yale University|Massey Cancer Center|Sidney Kimmel Comprehensive Cancer Center October 2016 Phase 1
NCT02905994 Not yet recruiting AML Massachusetts General Hospital|Boehringer Ingelheim September 2016 Phase 1
NCT02861040 Withdrawn Recurrent Adult Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia Northwestern University|National Comprehensive Cancer Network|National Cancer Institute (NCI) August 2016 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID