2. Cell Cycle/DNA Damage Apoptosis Cytoskeleton
  3. Microtubule/Tubulin Apoptosis Mitosis
  4. Estramustine

Estramustine, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer.

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Estramustine

Estramustine 構造式

CAS 番号 : 2998-57-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $80 在庫あり
25 mg $160 在庫あり
50 mg $260 在庫あり
100 mg $420 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Other Forms of Estramustine:

Estramustine 関連抗体

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製品説明

Estramustine, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer[1][2][3].

IC50 & Target

Tubulin 1[1]
Cellular Effect
Cell Line Type Value Description References
HeLa IC50
3.4 x 10-6 41
Compound: estramustine
Compound was evaluated for toxicity against HeLa S3 cells
Compound was evaluated for toxicity against HeLa S3 cells
[PMID: 3735321]
体外実験

Estramustine (1 µg/mL, 48 h) suppresses PC3 cell growth[1].
Estramustine (2 µg/mL, 48 h) elevates phosphatidylserine eversion amount on PC3 cells and induces PC3 cell apoptosis through reducing miR-31[1].
Estramustine (0-40 µM, 24-72 h) inhibits cell proliferation and tubulin cytoskeleton in RAW 264.7 cells[2].
Estramustine (10 µM, 24 h) inhibits TGF-β-induced RAW 264.7 cell migration, as well as TGF-β-induced uPA production by inhibiting Smad3 activation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Estramustine 関連抗体

Cell Viability Assay[1]

Cell Line: PC3 cells
Concentration: 1 µg/ mL
Incubation Time: 48 h
Result: Suppressed PC3 cell growth.

Immunofluorescence[2]

Cell Line: RAW 264.7 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Disrupted the interphase microtubules.

Cell Migration Assay [2]

Cell Line: 18 h of TGF-β treated RAW 264.7 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Inhibited TGF-β-Induced Cell Migration.
体内実験

Estramustine (Intraperitoneal injection, 4 or 12 mg/kg, a daily dose for 2 weeks) inhibits PAC120 tumor growth 53% by day 35[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Human prostate cancer xenograft PAC120[3]
Dosage: 4 or 12 mg/kg, a daily dose for 2 weeks.
Administration: Intraperitoneal injection
Result: Inhibited PAC120 tumor growth 53% by day 35.
臨床実験
分子量

440.40

分子式

C23H31Cl2NO3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](CC[C@@H]2O)([H])[C@@]3([H])[C@@](CC1)([H])C4=CC=C(OC(N(CCCl)CCCl)=O)C=C4CC3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (227.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2707 mL 11.3533 mL 22.7066 mL
5 mM 0.4541 mL 2.2707 mL 4.5413 mL
10 mM 0.2271 mL 1.1353 mL 2.2707 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.15%

COA (248 KB) HNMR (270 KB) LCMS (89 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2707 mL 11.3533 mL 22.7066 mL 56.7666 mL
5 mM 0.4541 mL 2.2707 mL 4.5413 mL 11.3533 mL
10 mM 0.2271 mL 1.1353 mL 2.2707 mL 5.6767 mL
15 mM 0.1514 mL 0.7569 mL 1.5138 mL 3.7844 mL
20 mM 0.1135 mL 0.5677 mL 1.1353 mL 2.8383 mL
25 mM 0.0908 mL 0.4541 mL 0.9083 mL 2.2707 mL
30 mM 0.0757 mL 0.3784 mL 0.7569 mL 1.8922 mL
40 mM 0.0568 mL 0.2838 mL 0.5677 mL 1.4192 mL
50 mM 0.0454 mL 0.2271 mL 0.4541 mL 1.1353 mL
60 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9461 mL
80 mM 0.0284 mL 0.1419 mL 0.2838 mL 0.7096 mL
100 mM 0.0227 mL 0.1135 mL 0.2271 mL 0.5677 mL
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Estramustine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

Estramustine2998-57-4Microtubule/TubulinApoptosisMitosisantineoplasticantimitoticdepolymerizationprostate tumorInhibitorinhibitorinhibit

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製品番号:
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