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

Ixabepilone (Synonyms: Azaepothilone B; BMS 247550; BMS 247550-1)

Cat. No.: HY-10222
Handling Instructions

Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.

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

Ixabepilone Chemical Structure

CAS No. : 219989-84-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $279 In-stock
5 mg $250 In-stock
10 mg $440 In-stock
50 mg $1500 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.

In Vitro

BMS-247550 is a highly potent cytotoxic agent capable of killing cancer cells at low nanomolar concentrations and retains its antineoplastic activity against human cancers that are naturally insensitive to paclitaxel or that have developed resistance to paclitaxel[1].

In Vivo

BMS-247550 demonstrates antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumors. BMS-247550 is more efficacious than paclitaxel in all five paclitaxel-resistant tumors evaluated in this study (four human and one murine): the clinically derived paclitaxel resistant Pat-7 ovarian carcinoma, the A2780Tax ovarian carcinoma that is resistant to paclitaxel because of tubulin mutations, the HCT116/VM46 MDR colon carcinoma, the clinically derived paclitaxel-resistant Pat-21 breast carcinoma, and the murine fibrosarcoma M5076. Against three paclitaxel-sensitive human tumor xenografts, BMS-247550 produces antitumor activity equivalent to paclitaxel: A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma[1].

Clinical Trial
Sponsor Condition Start Date Phase
Bristol-Myers Squibb Co Endometrioid carcinoma 2009-08-31 Phase 3
Federation Nationale des Centres de Lutte Contre le Cancer Breast tumor 2007-09-30 Phase 3
Bristol-Myers Squibb Co Metastatic breast cancer 2003-09-30 Phase 3
Sarah Cannon Research Institute Breast tumor 2009-01-31 Phase 3
Cancer and Leukemia Group B Metastatic breast cancer 2008-10-31 Phase 3
References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9736 mL 9.8678 mL 19.7355 mL
5 mM 0.3947 mL 1.9736 mL 3.9471 mL
10 mM 0.1974 mL 0.9868 mL 1.9736 mL
Kinase Assay
[1]

The potency with which BMS-247550 and paclitaxel polymerize tubulin isolated from calf brain is evaluated by Published techniques. Briefly, different concentrations of paclitaxel or BMS-247550 in polymerization buffer [0.1 M mes, 1 mM EGTA, 0.5 mM MgCl2 (pH 6.6)] are added to tubulin in polymerization buffer at 37°C in microcuvette wells of a Beckman. Model DU 7400 UV spectrophotometer. A final microtubule protein concentration of 1.0 mg/mL and compound concentrations of generally 2.5, 5.0, and 10 μM are used. Initial slopes of absorbance (A280 nM) change, measured every 10 s, are calculated by the software program accompanying the instrument.

Cell Assay
[1]

BMS-247550 is dissolved in 100% DMSO.

HCT116 cells from cultures are collected by trypsinization after 1, 2, 4, 8, 16, and 24 h exposure to 7.5 nm of BMS-247550. Cells are pelleted and fixed in 80% ethanol at −20°C. After an overnight storage at −20°C, cells are rehydrated with PBS buffer and DNA stain by incubation with propidium iodide (5 μg/mL) in 0.1% RNase for 15-30 min. Fluorescence-activated cell sorter acquisition is performed using the FACS Calibur instrument and analysis is done using Cellquest and Modfit software.

References
M.Wt

506.7

Formula

C₂₇H₄₂N₂O₅S

CAS No.

219989-84-1

Storage
Powder -20°C 3 years
  4°C 2 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

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:
Ixabepilone
Cat. No.:
HY-10222
Quantity: