Referencia número: HY-15278

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Utidelone

(Synonyms: Epothilone D; UTD1; KOS 862)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Utidelone (Epothilone D) is a potent microtubule stabilizer.

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Pureza: 99.67%
No. CAS: 189453-10-9
Fòrmula: C₂₇H₄₁NO₅S
Peso molecular:491.68

Almacenamiento:

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

Utidelone Chemical Structure

No. CAS: 189453-10-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (4)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Utidelone (Epothilone D) is a potent microtubule stabilizer.

IC₅₀ & Target

Microtubule/Tubulin^[1]

Ver todos los productos específicos de isoformas Antibiotic :

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]
L929	IC₅₀	20 ng/mL Compound: 15	Cytotoxicity against mouse L929 cells Cytotoxicity against mouse L929 cells	[PMID: 11473410]
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

Utidelone (Epothilone D) is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Utidelone has shown potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. Utidelone 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].
Utidelone 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 Utidelone (Epothilone D) improves MT and axonal function in PS19 mice, groups of 3-month old male PS19 mice received weekly i.p. injections of vehicle or Utidelone (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 Utidelone or vehicle. The 3 mg/kg Utidelone 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 Utidelone 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 Utidelone-treated mice. The motor performance of Utidelone-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 Utidelone 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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 189453-10-9
Appearance Solid
Peso molecular 491.68
Fòrmula C₂₇H₄₁NO₅S
Color White to light yellow
SMILES

O=C1C[C@H](O)C(C)(C)C([C@H](C)[C@@H](O)[C@@H](C)CCC/C(C)=C/C[C@@H](/C(C)=C/C2=CSC(C)=N2)O1)=O
Synonyms

Epothilone D; UTD1; KOS 862
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (4)

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Sci Rep

Enhancing microtubule stabilization rescues cognitive deficits and ameliorates pathological phenotype in an amyloidogenic Alzheimer's disease model. [Abstract]

2020 Sep 8;10(1):14776. PMID: 32901091
Front Mol Neurosci

Deleterious and protective effects of epothilone-D alone and in the context of amyloid β- and tau-induced alterations. [Abstract]

2023 Oct 12:16:1198299. PMID: 37900942
bioRxiv

2025 Nov 12.
Harvard University

2019 May.

Solvente y solubilidad

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocolo

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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Utidelone

4 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Utidelone

Ver todos los productos específicos de isoformas Antibiotic

Actividad biológica

Chemical Information

Publications (4)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Utidelone

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Lipid Compound Library

Antifungal Compound Library

Antibacterial Compound Library

Cytoskeleton Compound Library

Antibiotics Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) Utidelone

Ver todos los productos específicos de isoformas Antibiotic

Actividad biológica

Chemical Information

Publications (4)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Utidelone Related Classifications

HY-15278 Related Classifications