Patupilone (Epothilone B)

別名: EPO906 中文名稱：埃博霉素B，帕土匹龍

目錄號(hào)：S1364 Purity: 99.95%

Patupilone (EPO906, Epothilone B)是一種紫杉醇樣microtubule穩(wěn)定劑，EC_0.01為1.8 μM。Phase 2。

Patupilone (Epothilone B) Chemical Structure

CAS: 152044-54-7

規(guī)格	價(jià)格	庫(kù)存
2mg	810.81	現(xiàn)貨
5mg	972.58	現(xiàn)貨
25mg	3867.62	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.95%

99.95

Patupilone (Epothilone B)相關(guān)產(chǎn)品

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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

Patupilone (EPO906, Epothilone B)是一種紫杉醇樣microtubule穩(wěn)定劑，EC_0.01為1.8 μM。Phase 2。

特性

Epothilone B是類似紫杉醇的抗癌常規(guī)化合物，誘導(dǎo)微管蛋白聚合。

靶點(diǎn)

Tubulin ^[1]
(Cell-free assay)

1.8 μM(EC0.01)

體外研究(In Vitro)
體外研究活性	Epothilone B 比 Epothilone A活性高。Epothilone B 的EC0.01為1.8 nM。Epothilone B 作用于HCT116細(xì)胞，有效抑制細(xì)胞增殖，IC50為0.8 nM。^[1] Epothilone B 作用于KB3-1, KBV-1, Hela,和 Hs578T細(xì)胞，誘導(dǎo)細(xì)胞周期停頓，且具有細(xì)胞毒性，IC50為3 nM 到92 nM。Epothilone B與紫杉醇競(jìng)爭(zhēng)性與微管結(jié)合,IC50為3.3 μM。^[2] 3.5 nM Epothilone B 作用于過(guò)量表達(dá)GFP-α-微管蛋白的MCF-7細(xì)胞，充分抑制微管動(dòng)力學(xué)。同時(shí)，Epothilone B誘導(dǎo)有絲分裂停滯，IC50 為3.5 nM。^[3] Epothilone B 作用于多發(fā)性骨髓瘤(MM)細(xì)胞,包括RPMI 8226, U266, MM.1S, LR5,和 MR20,直接抑制細(xì)胞增殖,IC50為1 nM到 10 nM。10 nM Epothilone B也誘導(dǎo)細(xì)胞周期停滯和細(xì)胞凋亡。 ^[4]最新研究顯示, 5 nM–100 nM Epothilone B作用于卵巢癌 Hey細(xì)胞,增強(qiáng)表面上皮細(xì)胞粘附抗原(EpCAM)。^[5]
激酶實(shí)驗(yàn)	微管蛋白聚合實(shí)驗(yàn)
激酶實(shí)驗(yàn)	純化牛腦微管蛋白(MTP), 包含約15%–20%微管相關(guān)蛋白。用于 Epothilone B-微管研究的buffer (MES buffer)含 0.1 M 2-嗎啉乙磺酸(MES), 1 mM EGTA, 0.5 mM MgCl₂, 和3 M 甘油，pH 為6.6。電子顯微鏡觀察的樣本置于碳覆蓋火棉膠片包被的網(wǎng)格上(300 個(gè)網(wǎng)孔)，用2%乙酸鈾酰進(jìn)行負(fù)染色。在有或無(wú)Epothilone B存在時(shí)，使用分光光度計(jì)和恒溫調(diào)節(jié)液體循環(huán)器。檢測(cè)微管裝配。溫度維持在35^oC，350 nm處檢測(cè)到變渾濁狀態(tài)(代表聚合物規(guī)模)。計(jì)算EC0.01。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	KB3-1, KBV-1, Hela, 和Hs578T細(xì)胞
	濃度	0–1 μM
	孵育時(shí)間	24 小時(shí)測(cè)定有絲分裂停頓,72 小時(shí)測(cè)定細(xì)胞毒性。
	方法	為了測(cè)定有絲分裂受阻和畸變，細(xì)胞接種在48孔板中(用臺(tái)酚藍(lán)染色，測(cè)定細(xì)胞數(shù))或置于蓋玻片上。24小時(shí)后,用 Epothilone B處理細(xì)胞，在固定時(shí)間間隔記錄。為了分析毒性, 測(cè)定細(xì)胞數(shù)，用臺(tái)酚藍(lán)染色記錄陽(yáng)性和陰性。同時(shí), 蓋玻片和培養(yǎng)基上清液中等分的細(xì)胞混合，用溶于PBS的Hoechst 33342 染色。在有絲分裂受阻（停在G2-M期）和畸變的時(shí)候記錄細(xì)胞。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Epothilone B 按 2.5 mg/kg–4 mg/kg 劑量作用于攜帶RPMI 8226細(xì)胞移植瘤的小鼠，延長(zhǎng)小鼠壽命且抑制腫瘤生長(zhǎng)。^[4]Epothilone B 作用于攜帶前列腺癌細(xì)胞，包括DU145和PC3的移植瘤小鼠，也抑制腫瘤生長(zhǎng)。^[6]
動(dòng)物實(shí)驗(yàn)	Animal Models	攜帶RPMI 8226 細(xì)胞移植瘤的小鼠
	Dosages	2.5 mg/kg–4 mg/kg
	Administration	靜脈注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
[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 [7] Swindell CS, et al. J Med Chem, 1991, 34(3), 1176-1184. + 展開(kāi)

參考文獻(xiàn)

[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
[7] Swindell CS, et al. J Med Chem, 1991, 34(3), 1176-1184.

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	507.68	分子式	C₂₇H₄₁NO₆S
CAS號(hào)	152044-54-7	SDF	Download Patupilone (Epothilone B) SDF
Smiles	CC1CCCC2(C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 102 mg/mL ( (200.91 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 102 mg/mL (200.91 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (196.97 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 100 mg/mL (196.97 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項(xiàng)

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):

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