Patupilone (Epothilone B)

Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 1.8 μM. Phase 2.

CAS No. 152044-54-7

サイズ	価格(税別)	在庫状況
2mg	JPY 16200	国内在庫あり
5mg	JPY 21900	国内在庫あり
25mg	JPY 80000	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个实验数据

製品安全説明書

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Patupilone (Epothilone B)関連製品

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シグナル伝達経路

Microtubule Associatedシグナル伝達経路

Microtubule Associated阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
KB-8511 cells	Growth inhibition assay	72 h	Concentration required to inhibit the growth of paclitaxel-resistant human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure), IC50=0.18 μM	11133086
KB-31 cells	Growth inhibition assay	72 h	Concentration required to inhibit the growth of paclitaxel-sensitive human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure)	11133086
human Bel7402	Proliferation assay	72 h	Antiproliferative activity against human Bel7402 after 72 hrs by CellTiter Glo assay, IC50=0.9 μM	22320354
ovarian carcinoma 1A9 cell	Growth inhibition assay		Inhibitory concentration against ovarian carcinoma 1A9 cell growth	16134928
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 A431 cell	Growth inhibition assay		Inhibition of human A431 cell growth in a cell viability assay, IC50=9.86e-06 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 Daoy cell	Growth inhibition assay		Inhibition of human Daoy cell growth in a cell viability assay， IC50=2.73e-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 A375 cell	Growth inhibition assay		Inhibition of human A375 cell growth in a cell viability assay, IC50=5e-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 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 HLE cell	Growth inhibition assay		Inhibition of human HLE cell growth in a cell viability assay, IC50=8.26e-05 μM	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 786-0 cell	Growth inhibition assay		Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.11 nM	SANGER
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 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
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 IGROV-1 cell	Growth inhibition assay		Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.156 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 SIG-M5 cell	Growth inhibition assay		Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=0.169 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 PSN1 cell	Growth inhibition assay		Inhibition of human PSN1 cell growth in a cell viability assay, IC50=0.173 μM	SANGER
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 BHY cell	Growth inhibition assay		Inhibition of human BHY cell growth in a cell viability assay, IC50=0.195 nM	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 HOS cell	Growth inhibition assay		Inhibition of human HOS cell growth in a cell viability assay, IC50=0.215 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 ES1 cell	Growth inhibition assay		Inhibition of human ES1 cell growth in a cell viability assay, IC50=0.221 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 LXF-289 cell	Growth inhibition assay		Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=0.277 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 T84 cell	Growth inhibition assay		Inhibition of human T84 cell growth in a cell viability assay, IC50=0.24 μM	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 LCLC-103H cell	Growth inhibition assay		Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=0.31 nM	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 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-H460 cell	Growth inhibition assay		Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=0.333 μM	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 HSC-2 cell	Growth inhibition assay		Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=0.363 nM	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 HMV-II cell	Growth inhibition assay		Inhibition of human HMV-II cell growth in a cell viability assay, IC50=0.394 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 NCI-H2122 cell	Growth inhibition assay		Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=0.41 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 SW954 cell	Growth inhibition assay		Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.436 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 KYSE-270 cell	Growth inhibition assay		Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=0.445 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 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 SW620 cell	Growth inhibition assay		Inhibition of human SW620 cell growth in a cell viability assay, IC50=0.648 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 DU-145 cell	Growth inhibition assay		Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.721 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 A427 cell	Growth inhibition assay		Inhibition of human A427 cell growth in a cell viability assay, IC50=0.828 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 NCI-H2009 cell	Growth inhibition assay		Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=0.862 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 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 EC_0.01 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 EC_0.01 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
Kinase 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, 0.5 mM MgCl₂, and 3 M glycerol 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 (EC_0.01), defined as the interpolated concentration capable of inducing an initial slope of 0.01 OD/min rate, is calculated using the formula EC_0.01 = 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 trypan 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 trypan 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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[1] Regueiro-Ren A , et al. Org Lett, 2001, 3(17), 2693-2696. [2] Bollag DM, et al. Cancer Res, 1995, 55(11), 2325-2333. [3] Kamath K, et al. Cancer Res, 2003, 63(18), 6026-6031. [4] Lin B, et al. Blood, 2005, 105(1), 350-357. [5] Shahabi S, et al. Gynecol Oncol, 2010, 119(2), 345-350. [6] O'Reilly T, et al. Prostate, 2005, 65(3), 231-240. [7] Swindell CS, et al. J Med Chem, 1991, 34(3), 1176-1184. + 展開

参考

+ 展開

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

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):