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Epothilone D

Epothilone D
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Epothilone D

Catalog No. TQ0202Cas No. 189453-10-9
Epothilone D (KOS 862) is an effective microtubule stabilizer.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$9706-8 weeks
50 mg$1,8506-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
Description
Epothilone D (KOS 862) is an effective microtubule stabilizer.
In vitro
Epothilone D 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].
In vivo
To evaluate whether 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 Epothilone D (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 or vehicle. The 3 mg/kg Epothilone D dose corresponds to ~10-fold less than that used in 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 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-treated mice. The motor performance of Epothilone D-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts [2].
Animal Research
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 the 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 [2].
AliasKOS 862
Chemical Properties
Molecular Weight491.68
FormulaC27H41NO5S
Cas No.189453-10-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 300 mg/mL (610.15 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0338 mL10.1692 mL20.3384 mL101.6922 mL
5 mM0.4068 mL2.0338 mL4.0677 mL20.3384 mL
10 mM0.2034 mL1.0169 mL2.0338 mL10.1692 mL
20 mM0.1017 mL0.5085 mL1.0169 mL5.0846 mL
50 mM0.0407 mL0.2034 mL0.4068 mL2.0338 mL
100 mM0.0203 mL0.1017 mL0.2034 mL1.0169 mL

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