Epothilone A (Synonyms: Epo A)

Name: Epothilone A
Brand: MedChemExpress
SKU: HY-13503
Rating: 4.5 (1 reviews)

Cat. No.: HY-13503 Purity: 98.60%: FAQs
Data Sheet SDS COA Handling Instructions

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Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers, with a K_i of 0.6-1.4 μM.

For research use only. We do not sell to patients.

Epothilone A Chemical Structure

CAS No. : 152044-53-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Epothilone A:

Epothilone A (Standard) Get quote

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Biological Activity
Purity & Documentation
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Description

Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers, with a K_i of 0.6-1.4 μM.

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 5 μM Compound: 4	Cytotoxicity against human A549 cells after 48 hrs by SRB assay Cytotoxicity against human A549 cells after 48 hrs by SRB assay	[PMID: 25084144]
A549	IC₅₀	2.2 nM Compound: Epo A	Antiproliferative activity against human A549 cells after 72 hrs Antiproliferative activity against human A549 cells after 72 hrs	[PMID: 19433359]
A549	IC₅₀	2.6 nM Compound: EpoA	Cytotoxicity against human A549 cells after 72 hrs by methylene blue assay Cytotoxicity against human A549 cells after 72 hrs by methylene blue assay	[PMID: 19804980]
HCT-116	IC₅₀	2.8 nM Compound: 1a, epothilone A	Antiproliferative activity against human HCT116 cells after 72 hrs by methylene blue staining Antiproliferative activity against human HCT116 cells after 72 hrs by methylene blue staining	[PMID: 18271516]
HT-1080	IC₅₀	1.3 nM Compound: EpoA	Cytotoxicity against human HT1080 cells after 3 days by MTT assay Cytotoxicity against human HT1080 cells after 3 days by MTT assay	[PMID: 19804980]
KB	IC₅₀	1.91 nM Compound: Epothilone A	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	0.0096 μM Compound: Epothilone A	Cytotoxicity against human KB3-1 cells by MTT assay Cytotoxicity against human KB3-1 cells by MTT assay	[PMID: 25397992]
KB 3-1	IC₅₀	2.15 nM Compound: Epothilone A	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]
L929	IC₅₀	0.0038 μM Compound: Epothilone A	Cytotoxicity against mouse L929 cells after 5 days by MTT assay Cytotoxicity against mouse L929 cells after 5 days by MTT assay	[PMID: 27231731]
L929	IC₅₀	0.0077 μM Compound: Epothilone A	Cytotoxicity against mouse L929 cells by MTT assay Cytotoxicity against mouse L929 cells by MTT assay	[PMID: 25397992]
MCF7	IC₅₀	0.0008 μM Compound: 4	Cytotoxicity against human MCF7 cells in presence of 10 mM DTT after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells in presence of 10 mM DTT after 48 hrs by SRB assay	[PMID: 25084144]
MCF7	IC₅₀	0.0009 μM Compound: 4	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 25084144]
MCF7	IC₅₀	0.0022 μM Compound: Epothilone A	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 25397992]
MCF7	IC₅₀	2.5 nM Compound: EpoA	Cytotoxicity against human MCF7 cells after 72 hrs by methylene blue assay Cytotoxicity against human MCF7 cells after 72 hrs by methylene blue assay	[PMID: 19804980]
MCF7	IC₅₀	2.6 nM Compound: Epo A	Antiproliferative activity against human MCF7 cells after 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs	[PMID: 19433359]
MCF7	IC₅₀	2.9 nM Compound: 1a, epothilone A	Antiproliferative activity against human MCF7 cells after 72 hrs by methylene blue staining Antiproliferative activity against human MCF7 cells after 72 hrs by methylene blue staining	[PMID: 18271516]
PC-3	IC₅₀	0.0024 μM Compound: Epothilone A	Cytotoxicity against human PC3 cells by MTT assay Cytotoxicity against human PC3 cells by MTT assay	[PMID: 25397992]
PC-3M	IC₅₀	6.4 nM Compound: 1a, epothilone A	Antiproliferative activity against human PC3M cells after 72 hrs by methylene blue staining Antiproliferative activity against human PC3M cells after 72 hrs by methylene blue staining	[PMID: 18271516]
SK-OV-3	IC₅₀	0.0013 μM Compound: Epothilone A	Cytotoxicity against human SKOV3 cells by MTT assay Cytotoxicity against human SKOV3 cells by MTT assay	[PMID: 25397992]

In Vitro

Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers. The apparent K_i value for Epothilone A is 1.4 μM by Hanes analysis and 0.6 μM by Dixon analysis^[1]. Epothilone A, is noted to be highly cytotoxic (IC₅₀=0.05 μM) in vitro when applied to the human T-24 bladder carcinoma cell line. The binding affinity of Epothilone A to tubulin is of the same order of magnitude as the binding affinity of paclitaxel to tubulin based on competition assays. The IC₅₀ for displacement of 100 nM of (³H) paclitaxel from the tubulin binding site is 3.6 μM for paclitaxel, 2.3 μM for Epothilone A, and 3.3 μM for patupilone^[2].

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

Molecular Weight

493.66

Formula

C₂₆H₃₉NO₆S

CAS No.

152044-53-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(C[C@H](O)C1(C)C)O[C@H](/C(C)=C/C2=CSC(C)=N2)C[C@]3([H])O[C@]3([H])CCC[C@H](C)[C@H](O)[C@@H](C)C1=O

Structure Classification

Initial Source

Microorganisms

Sorangium cellulosum

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (253.21 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	2.0257 mL	10.1284 mL	20.2569 mL
5 mM	0.4051 mL	2.0257 mL	4.0514 mL
10 mM	0.2026 mL	1.0128 mL	2.0257 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. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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.

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (261 KB) HNMR (205 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Kowalski RJ, et al. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)). J Biol Chem. 1997 Jan 24;272(4):2534-41. [Content Brief]

[2]. Cheng KL, et al. Novel microtubule-targeting agents - the epothilones. Biologics. 2008 Dec;2(4):789-811. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0257 mL	10.1284 mL	20.2569 mL	50.6421 mL
	5 mM	0.4051 mL	2.0257 mL	4.0514 mL	10.1284 mL
	10 mM	0.2026 mL	1.0128 mL	2.0257 mL	5.0642 mL
	15 mM	0.1350 mL	0.6752 mL	1.3505 mL	3.3761 mL
	20 mM	0.1013 mL	0.5064 mL	1.0128 mL	2.5321 mL
	25 mM	0.0810 mL	0.4051 mL	0.8103 mL	2.0257 mL
	30 mM	0.0675 mL	0.3376 mL	0.6752 mL	1.6881 mL
	40 mM	0.0506 mL	0.2532 mL	0.5064 mL	1.2661 mL
	50 mM	0.0405 mL	0.2026 mL	0.4051 mL	1.0128 mL
	60 mM	0.0338 mL	0.1688 mL	0.3376 mL	0.8440 mL
	80 mM	0.0253 mL	0.1266 mL	0.2532 mL	0.6330 mL
	100 mM	0.0203 mL	0.1013 mL	0.2026 mL	0.5064 mL

Epothilone A Related Classifications

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:

Epothilone A152044-53-6Epo AMicrotubule/TubulinApoptosisInhibitorinhibitorinhibit

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Epothilone A (Synonyms: Epo A)

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