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Epothilone A Microtubule Associated inhibitor

Name: Epothilone A
Brand: Selleck Chemicals
SKU: S1297
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S1297

Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 2 μM.

Chemical Structure

Molecular Weight: 493.66

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.10%

99.10

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Chemical Information, Storage & Stability

Molecular Weight	493.66	Formula	C₂₆H₃₉NO₆S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	152044-53-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1CCCC2C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (200.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 99 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (1.27mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Tubulin ^[1] 2 μM(EC0.01)
In vitro	Epothilone A, discovered from the myxobacterium Sorangium cellulosum, is a Taxol-like microtubule-stabilizing agent that induces tubulin polymerization, leading to cell cycle arrest at the G2-M transition, cytotoxicity, and apoptosis. This compound potently inhibits cell proliferation in HCT116 cells, with IC50 of 4.4 nM. ^[1] It also displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 values ranging from 13 nM to 160 nM. This chemical is more water soluble than Taxol and competes with Taxol in binding with microtubules, with IC50 of 2.3 μM. ^[2] However, both this compound and Taxol don't share a common pharmacophore and exploits the tubulin-binding pocket uniquely and independently. ^[3] Recently, it is found that microbiological transformation of this compound by Aspergillus niger AS 3.739 yields several metabolites that is also toxic to MCF-7 cells, but with much higher IC50 values. ^[4]
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 A-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 this compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11506611/ [2] https://pubmed.ncbi.nlm.nih.gov/7757983/ [3] https://pubmed.ncbi.nlm.nih.gov/15297674/ [4] https://pubmed.ncbi.nlm.nih.gov/19431017/ [5] https://pubmed.ncbi.nlm.nih.gov/1672157/

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