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  2. Cell Cycle/DNA Damage Cytoskeleton Anti-infection
  3. Microtubule/Tubulin Fungal Bacterial Antibiotic
  4. Epothilone D

Epothilone D  (Synonyms: 埃博霉素; KOS 862)

目錄號(hào): HY-15278 純度: 99.82%
COA 產(chǎn)品使用指南 技術(shù)支持

Epothilone D (KOS 862) 是有效的微管穩(wěn)定劑。

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Epothilone D Chemical Structure

Epothilone D Chemical Structure

CAS No. : 189453-10-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2110
In-stock
2 mg ￥900
In-stock
5 mg ￥1950
In-stock
10 mg ￥3200
In-stock
25 mg 現(xiàn)貨 詢價(jià)
50 mg   詢價(jià)  
100 mg   詢價(jià)  

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Customer Review

Other Forms of Epothilone D:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Epothilone D (KOS 862) is a potent microtubule stabilizer.

IC50 & Target

Microtubule/Tubulin[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM IC50
15 nM
Compound: 4
Cytotoxicity against camptothecin-resistant human CCRF-CEM cells after 3 days by SRB assay
Cytotoxicity against camptothecin-resistant human CCRF-CEM cells after 3 days by SRB assay
[PMID: 12141877]
CCRF-CEM IC50
22 nM
Compound: 4
Cytotoxicity against human CCRF-CEM cells after 3 days by SRB assay
Cytotoxicity against human CCRF-CEM cells after 3 days by SRB assay
[PMID: 12141877]
HL-60 IC50
10 nM
Compound: 4
Cytotoxicity against mitoxantrone-resistant human HL60 cells after 3 days by SRB assay
Cytotoxicity against mitoxantrone-resistant human HL60 cells after 3 days by SRB assay
[PMID: 12141877]
HL-60 IC50
8 nM
Compound: 4
Cytotoxicity against human HL60 cells after 3 days by SRB assay
Cytotoxicity against human HL60 cells after 3 days by SRB assay
[PMID: 12141877]
KB IC50
1.44 nM
Compound: Epothilone D
Concentration required to inhibit the growth of paclitaxel-resistant human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure)
Concentration required to inhibit the growth of paclitaxel-resistant human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure)
[PMID: 11133086]
KB 3-1 IC50
2.7 nM
Compound: Epothilone D
Concentration required to inhibit the growth of paclitaxel-sensitive human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure)
Concentration required to inhibit the growth of paclitaxel-sensitive human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure)
[PMID: 11133086]
MCF7 IC50
0.014 μM
Compound: Epo D
Cytotoxicity against human MCF7 cells after 72 hrs
Cytotoxicity against human MCF7 cells after 72 hrs
[PMID: 23994325]
MCF7 IC50
16 nM
Compound: 4
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
[PMID: 14575429]
MCF7 IC50
8 nM
Compound: 4
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
[PMID: 12141877]
NCI/ADR-RES IC50
0.01 μM
Compound: Epo D
Cytotoxicity against human MCF7/ADR cells after 72 hrs
Cytotoxicity against human MCF7/ADR cells after 72 hrs
[PMID: 23994325]
NCI/ADR-RES IC50
30 nM
Compound: 4
Cytotoxicity against human NCI/ADR-RES cells after 3 days by SRB assay
Cytotoxicity against human NCI/ADR-RES cells after 3 days by SRB assay
[PMID: 12141877]
NCI-H460 IC50
30 nM
Compound: 4
Cytotoxicity against human NCI-H460 cells after 3 days by SRB assay
Cytotoxicity against human NCI-H460 cells after 3 days by SRB assay
[PMID: 14575429]
NCI-H460 IC50
8 nM
Compound: 4
Cytotoxicity against human NCI-H460 cells after 3 days by SRB assay
Cytotoxicity against human NCI-H460 cells after 3 days by SRB assay
[PMID: 12141877]
SF-268 IC50
14 nM
Compound: 4
Cytotoxicity against human SF268 cells after 3 days by SRB assay
Cytotoxicity against human SF268 cells after 3 days by SRB assay
[PMID: 12141877]
SF-268 IC50
18 nM
Compound: 4
Cytotoxicity against human SF268 cells after 3 days by SRB assay
Cytotoxicity against human SF268 cells after 3 days by SRB assay
[PMID: 14575429]
體外研究
(In Vitro)

Epothilone D (KOS-862) is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Epothilone D has shown potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. Epothilone D also shows a definite advantage over paclitaxel in drug-resistant cell lines, and retained its cytotoxicity against a multidrug resistant cell line over-expressing P-glycoprotein[1]. Epothilone D (EpoD) is a microtubules (MTs)-stabilizing agent[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

To evaluate whether Epothilone D (EpoD) improves MT and axonal function in PS19 mice, groups of 3-month old male PS19 mice received weekly i.p. injections of vehicle or Epothilone D (EpoD) (1 mg/kg or 3 mg/kg) for a total of 3 months. In addition, 3-month old non-Tg littermates received 3 mg/kg Epothilone D (EpoD) or vehicle. The 3 mg/kg Epothilone D (EpoD) dose corresponds to ~10-fold less than that used in a Phase II clinical study, which should minimize side-effects such as neutropenia that are observed with MT-stabilizing drugs in human subjects. PS19 and WT mice that receive Epothilone D (EpoD) show no signs of drug intolerance. Indeed, all drug-treated mice exhibited weight gain that is indistinguishable from vehicle-treated animals. Likewise, relative organ weights are similar in vehicle- and Epothilone D (EpoD)-treated mice. The motor performance of Epothilone D (EpoD)-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts. Finally, although there is minor group-to-group variability, there are no significant differences in white blood cell counts or neutrophil content between any of the treatment cohorts. Thus, the low doses of Epothilone D (EpoD) utilized in these studies appeared to be well tolerated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

491.68

Formula

C27H41NO5S
CAS 號(hào)
性狀

固體

顏色

White to light yellow

中文名稱

埃博霉素 D
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 100 mg/mL (203.38 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.0338 mL 10.1692 mL 20.3384 mL
5 mM 0.4068 mL 2.0338 mL 4.0677 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.93%

參考文獻(xiàn)
Animal Administration
[2]

Mice[2]
Groups of mice (n=3) receive intraperitoneal (i.p.) injections of 3.7 mg/kg of Epothilone D (epoD) dissolved in 100% DMSO, followed by euthanization using approved at times ranging from 0.25 h to 24 h. In another study, groups of mice (n=3) receive injections of 3 mg/kg of epoD in 100% DMSO followed by euthanization 4, 6 and 10 days later. The Epothilone D (epoD) levels in brain and blood samples are determined using LC-MS/MS protocols. Groups (n=10-13) of 3-month old PS19 tau Tg mice or 3-month old non-Tg littermates are administered weekly i.p. injections of 1 mg/kg epoD, 3 mg/kg of Epothilone D (epoD) or vehicle (DMSO), for a total of 3 months. Animals are monitored for signs of abnormal behavior or distress, and are weighed weekly. After final dosing, the mice undergo motor function and cognitive testing. After euthanization, brains and optic nerve (ON) are recovered for immunohistochemical analyses. A subset of mice from each group also undergo necropsy evaluation with organ weights recorded.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0338 mL 10.1692 mL 20.3384 mL 50.8461 mL
5 mM 0.4068 mL 2.0338 mL 4.0677 mL 10.1692 mL
10 mM 0.2034 mL 1.0169 mL 2.0338 mL 5.0846 mL
15 mM 0.1356 mL 0.6779 mL 1.3559 mL 3.3897 mL
20 mM 0.1017 mL 0.5085 mL 1.0169 mL 2.5423 mL
25 mM 0.0814 mL 0.4068 mL 0.8135 mL 2.0338 mL
30 mM 0.0678 mL 0.3390 mL 0.6779 mL 1.6949 mL
40 mM 0.0508 mL 0.2542 mL 0.5085 mL 1.2712 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0169 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8474 mL
80 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6356 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Epothilone D
目錄號(hào)：
HY-15278
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