Epothilone D (Synonyms: KOS 862)

Name: Epothilone D
Brand: MedChemExpress
SKU: HY-15278
Rating: 5.0 (3 reviews)

Cat. No.: HY-15278 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Epothilone D Chemical Structure

CAS No. : 189453-10-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 211	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 211	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 195	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 630	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1000	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 3 publication(s) in Google Scholar

Other Forms of Epothilone D:

(16R)-Epothilone D Get quote

3 Publications Citing Use of MCE Epothilone D

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

Microtubule/Tubulin^[1]

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]

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].

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

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].

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

Clinical Trial

Molecular Weight

491.68

Formula

C₂₇H₄₁NO₅S

CAS No.

189453-10-9

Appearance

Solid

Color

White to light yellow

SMILES

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

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 : ≥ 100 mg/mL (203.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2034 mL	1.0169 mL	2.0338 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: ≥ 2.5 mg/mL (5.08 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.93%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (260 KB) HNMR (214 KB) LCMS (351 KB) Elemental Analysis Report (117 KB)

Handling Instructions (2659 KB)

References

[1]. Konner J, et al. Phase I clinical, pharmacokinetic, and pharmacodynamic study of KOS-862 (Epothilone D) in patients with advanced solid tumors and lymphoma. Invest New Drugs. 2012 Dec;30(6):2294-302. [Content Brief]

[2]. Brunden KR, et al. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J Neurosci. 2010 Oct 13;30(41):13861-6. [Content Brief]

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.

References

[1]. Konner J, et al. Phase I clinical, pharmacokinetic, and pharmacodynamic study of KOS-862 (Epothilone D) in patients with advanced solid tumors and lymphoma. Invest New Drugs. 2012 Dec;30(6):2294-302. [Content Brief]

[2]. Brunden KR, et al. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J Neurosci. 2010 Oct 13;30(41):13861-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Epothilone D 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 D189453-10-9KOS 862KOS862KOS-862Microtubule/TubulinFungalBacterialAntibioticInhibitorinhibitorinhibit

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Epothilone D (Synonyms: KOS 862)

Customer Review

Other Forms of Epothilone D:

Epothilone D Related Antibodies

3 Publications Citing Use of MCE Epothilone D

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•Related Screening Libraries:

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View All Antibiotic Isoform Specific Products:

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Protocol

Purity & Documentation

References

Customer Review

Epothilone D Related Antibodies

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Complete Stock Solution Preparation Table

Epothilone D Related Classifications

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