1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

Epothilone D (Synonyms: 12,13-Desoxyepothilone B; Desoxyepothilone B; KOS 862)

Cat. No.: HY-15278 Purity: 99.86%
Handling Instructions

Epothilone D is a potent microtubule stabilizer.

For research use only. We do not sell to patients.
Epothilone D Chemical Structure

Epothilone D Chemical Structure

CAS No. : 189453-10-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $165 In-stock
5 mg $150 In-stock
10 mg $240 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Epothilone D is a potent microtubule stabilizer.

IC50 & Target

Microtubule/Tubulin[1]

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].

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 (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 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 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. 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 utilized in these studies appeared to be well tolerated[2].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Animal Administration
[2]

Epothilone D (EpoD) in 100% DMSO and diluted with saline or PBS (Mice)[2].

Mice[2]
Groups of mice (n=3) receive intraperitoneal (i.p.) injections of 3.7 mg/kg of 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 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 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.

References
M.Wt

491.68

Formula

C₂₇H₄₁NO₅S

CAS No.

189453-10-9

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 99.86%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Epothilone D
Cat. No.:
HY-15278
Quantity: