Patupilone (Epothilone B)

別名:EPO906

Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.

Patupilone (Epothilone B)化学構造

CAS No. 152044-54-7

サイズ 価格(税別) 在庫状況
JPY 29500 国内在庫あり
JPY 44500 国内在庫あり
JPY 88500 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(16)

カスタマーフィードバック4

製品安全説明書

現在のバッチを見る: 純度: 99.95%
99.95

Patupilone (Epothilone B)関連製品

Microtubule Associated阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human NCI-H2009 cell Growth inhibition assay Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=0.862 μM SANGER
human HT-1080 cell Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=0.842 μM SANGER
human A427 cell Growth inhibition assay Inhibition of human A427 cell growth in a cell viability assay, IC50=0.828 μM SANGER
human ST486 cell Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50=0.721 μM SANGER
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.721 μM SANGER
human HCT-15 cell Growth inhibition assay Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=0.717 μM SANGER
human SW620 cell Growth inhibition assay Inhibition of human SW620 cell growth in a cell viability assay, IC50=0.648 μM SANGER
human SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=0.646 μM SANGER
human NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=0.447 μM SANGER
human KYSE-270 cell Growth inhibition assay Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=0.445 μM SANGER
human SW954 cell Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.436 μM SANGER
human CAL-39 cell Growth inhibition assay Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=0.411 μM SANGER
human NCI-H2122 cell Growth inhibition assay Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=0.41 μM SANGER
human COLO-679 cell Growth inhibition assay Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=0.394 μM SANGER
human HMV-II cell Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=0.394 μM SANGER
human IA-LM cell Growth inhibition assay Inhibition of human IA-LM cell growth in a cell viability assay, IC50=0.393 μM SANGER
human HSC-2 cell Growth inhibition assay Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=0.363 nM SANGER
human HGC-27 cell Growth inhibition assay Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=0.338 μM SANGER
human NCI-H460 cell Growth inhibition assay Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=0.333 μM SANGER
human HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.328 μM SANGER
human NCI-H810 cell Growth inhibition assay Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.322 μM SANGER
human LCLC-103H cell Growth inhibition assay Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=0.31 nM SANGER
human KYSE-450 cell Growth inhibition assay Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50=0.267 μM SANGER
human T84 cell Growth inhibition assay Inhibition of human T84 cell growth in a cell viability assay, IC50=0.24 μM SANGER
human CAL-12T cell Growth inhibition assay Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=0.239 μM SANGER
human LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=0.277 μM SANGER
human TE-15 cell  Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.225 μM SANGER
human ES1 cell  Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=0.221 μM SANGER
human 639-V cell Growth inhibition assay Inhibition of human 639-V cell growth in a cell viability assay, IC50=0.218 μM SANGER
human HOS cell Growth inhibition assay Inhibition of human HOS cell growth in a cell viability assay, IC50=0.215 μM SANGER
human BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=0.201 μM SANGER
human BHY cell Growth inhibition assay Inhibition of human BHY cell growth in a cell viability assay, IC50=0.195 nM SANGER
KB-31 cells Growth inhibition assay 72 h Concentration required to inhibit the growth of human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure) 11133086
KB-8511 cells Growth inhibition assay 72 h Concentration required to inhibit the growth of human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure), IC50=0.18 μM 11133086
human PA-1 cell Growth inhibition assay Inhibition of human PA-1 cell growth in a cell viability assay, IC50=0.174 μM SANGER
human PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=0.173 μM SANGER
human NCI-H650 cell Growth inhibition assay Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=0.17 μM SANGER
human SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=0.169 μM SANGER
human MG-63 cell Growth inhibition assay Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.165 μM SANGER
human IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.156 μM SANGER
human VMRC-RCZ cell Growth inhibition assay Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.136 μM SANGER
human PANC-03-27 cell Growth inhibition assay Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=0.132 μM SANGER
ovarian carcinoma 1A9 cell Growth inhibition assay Inhibitory concentration against ovarian carcinoma 1A9 cell growth 16134928
human TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.111 nM SANGER
human 786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.11 nM SANGER
human MCF7 cell Growth inhibition assay Inhibition of human MCF7 cell growth in a cell viability assay, IC50=8.66e-05 μM SANGER
human HLE cell Growth inhibition assay Inhibition of human HLE cell growth in a cell viability assay, IC50=8.26e-05 μM SANGER
human KYSE-510 cell Growth inhibition assay Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=7.38e-05 μM SANGER
human RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=6.47e-05 μM SANGER
human A375 cell Growth inhibition assay Inhibition of human A375 cell growth in a cell viability assay, IC50=5e-05 μM SANGER
human BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=4.99e-05 μM SANGER
human Daoy cell Growth inhibition assay Inhibition of human Daoy cell growth in a cell viability assay, IC50=2.73e-05 μM SANGER
human SW1710 cell Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.14e-05 μM SANGER
human A431 cell Growth inhibition assay Inhibition of human A431 cell growth in a cell viability assay, IC50=9.86e-06 μM SANGER
human LC-2-ad cell Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=3.77e-06 μM SANGER
human LCLC-97TM1 cell Growth inhibition assay Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=0.444 μM SANGER
human SK-LU-1 cell Growth inhibition assay Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=0.866 μM SANGER
human SCC-4 cell Growth inhibition assay Inhibition of human SCC-4 cell growth in a cell viability assay, IC50=0.877 μM SANGER
human NCI-H1299 cell Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=0.88 μM SANGER
human NH-12 cell Growth inhibition assay Inhibition of human NH-12 cell growth in a cell viability assay, IC50=0.891 μM SANGER
human SK-UT-1 cell Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=0.892 μM SANGER
human Bel7402 Proliferation assay 72 h Antiproliferative activity against human Bel7402 after 72 hrs by CellTiter Glo assay, IC50=0.9 μM 22320354
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=0.94 μM SANGER
human SW982 cell Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.999 μM SANGER
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
Targets
Tubulin [1]
(Cell-free assay)
1.8 μM(EC0.01)
In Vitro
In vitro

Epothilone B shows better activity than Epothilone A. The EC0.01 of Epothilone B is 1.8 μM. Epothilone B potently inhibits cell proliferation in HCT116 cells, with IC50 of 0.8 nM. [1] Epothilone B induces mitotic arrest and displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 of 3 nM to 92 nM. Epothilone B competes with Taxol in binding to microtubules, with IC50 of 3.3 μM. [2] In MCF-7 cells overexpressing GFP-α-tubulin, Epothilone B (3.5 nM) efficiently blocks microtubule dynamics. Meanwhile, Epothilone B induces mitotic arrest with IC50 of 3.5 nM. [3] In multiple myeloma (MM) cells, including RPMI 8226, U266, MM.1S, LR5, and MR20, Epothilone B directly suppresses proliferation with IC50 of 1 nM to 10 nM. Similarly, Epothilone B (10 nM) also induces cell cycle arrest and apoptosis. [4] A recent study reveals that, in ovarian cancer Hey cells, Epothilone B (5 nM–100 nM) enhances surface epithelial cell adhesion antigen (EpCAM), without affecting the transcription or the total cellular level of EpCAM. [5]

Kinase Assay Tubulin polymerization assay
Calf brain microtubule proteins (MTP) are purified, which includes approximately 15%–20% microtubule associated proteins. The buffer (MES buffer) used for the Epothilone B-microtubule studies contains 0.1 M 2-morpholinoethanesulfonic acid (MES), 1 mM EGTA and 0.5 mM MgCl2 at pH 6.6. Samples for electron microscopy are placed on carbon-over-Parlodion-coated grids (300 mesh) and negatively stained with 2% uranyl acetate. Microtubule assembly in the presence or absence of Epothilone B is monitored spectrophotometrically by using a spectrophotometer equipped with a thermostatically regulated liquid circulator. The temperature is held at 35 °C and changes in turbidity (representative of polymer mass) are monitored at 350 nm. Effective concentration (EC0.01), defined as the interpolated concentration capable of inducing an initial slope of 0.01 OD/min rate, is calculated using the formula EC0.01 = concentration/slope and expressed as the mean with standard deviation obtained from three different concentrations.
細胞実験 細胞株 KB3-1, KBV-1, Hela, and Hs578T cells
濃度 0–1 μM
反応時間 72 hours
実験の流れ

For mitotic block and aberrant mitosis, cells are plated either in 48-well plates (for blue and cell counting) or onto coverslips. After 24 hours, cells are treated with Epothilone B and scored at regular intervals. For the cytotoxicity analysis, cells are counted and scored as blue positive or negative. Concurrently, coverslips andaliquots of cells in the culture supernatant are fixed and stained with Hoechst33342 in PBS. These cells are scored for cells blocked at the G2/M transition and aberrant mitosis.

In Vivo
In Vivo

In a mouse xenograft model of RPMI 8226 cells, Epothilone B (2.5 mg/kg–4 mg/kg) prolongs survival and suppresses tumor growth. [4] Similarly, in mouse xenograft models of prostate cancer cells, including DU145 and PC3, Epothilone B at the same dose also inhibits tumor growth. [6]

動物実験 動物モデル Mice xenograft model of RPMI 8226 cells
投与量 2.5 mg/kg–4 mg/kg
投与経路 Inject intravenously
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00496600 Completed
Refractory Malignancy
University of Medicine and Dentistry of New Jersey|Novartis Pharmaceuticals|National Cancer Institute (NCI)|Rutgers The State University of New Jersey
July 2007 Phase 1
NCT00442741 Withdrawn
Solid Tumors
Novartis Pharmaceuticals|Novartis
July 2007 Phase 1
NCT00468260 Terminated
Advanced Malignancies
Novartis Pharmaceuticals|Novartis
May 2007 Phase 1
NCT00448396 Completed
Advanced Malignancies
Novartis Pharmaceuticals|Novartis
March 2007 Phase 1
NCT00426140 Completed
Advanced Malignancies|Solid Tumors
Novartis Pharmaceuticals|Novartis
August 2006 Phase 1

化学情報

分子量 507.68 化学式

C27H41NO6S

CAS No. 152044-54-7 SDF Download Patupilone (Epothilone B) SDFをダウンロードする
Smiles CC1CCCC2(C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C
保管

In vitro
Batch:

DMSO : 102 mg/mL ( (200.91 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。)

Ethanol : 102 mg/mL

Water : 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

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

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: Patupilone (Epothilone B)を買う | Patupilone (Epothilone B) ic50 | Patupilone (Epothilone B)供給者 | Patupilone (Epothilone B)を購入する | Patupilone (Epothilone B)費用 | Patupilone (Epothilone B)生産者 | オーダーPatupilone (Epothilone B) | Patupilone (Epothilone B)化学構造 | Patupilone (Epothilone B)分子量 | Patupilone (Epothilone B)代理店