Home Cytoskeletal Signaling Microtubule Associated inhibitor Ixabepilone For research use only.

Ixabepilone

Synonyms: Azaepothilone B, BMS-247550, Aza-epothilone B

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

Ixabepilone Chemical Structure

Ixabepilone Chemical Structure

CAS No. 219989-84-1

Purity & Quality Control

Ixabepilone Related Products

Signaling Pathway

Microtubule Associated Signaling Pathways

Microtubule Associated Signaling Pathway

Biological Activity

Description Ixabepilone is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.
Targets
microtubule(tubulin stabilising) [1]
In vitro
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].
Cell Research Cell lines HCT116 human carcinoma cell lines
Concentrations 7.5 nM
Incubation Time 1, 2, 4, 8, 16, and 24 h
Method

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.
In Vivo
In vivo

In vivo, BMS-247550 has clearly demonstrated 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): i.e., 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: i.e., A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma[1].
Animal Research Animal Models Human tumor xenografts（BALB/c nu/nu nude mice）
Dosages various concentrations
Administration i.v. or p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03093155 Completed
Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer
Yale University|R-Pharm-US LLC
 April 3 2017 Phase 2
NCT01454479 Unknown status
Recurrent Endometrial Cancer
Hung-Hsueh Chou|GlaxoSmithKline|Bristol-Myers Squibb|Chang Gung Memorial Hospital
 March 2011 Phase 1
NCT01012362 Terminated
Breast Cancer|Lung Cancer|Colon Cancer|Pancreatic Cancer|Head and Neck Cancer|Kidney Cancer|Sarcoma|Hepatocellular Cancer
Masonic Cancer Center University of Minnesota|GlaxoSmithKline
 December 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 506.70 Formula

C27H42N2O5S
CAS No. 219989-84-1 SDF Download Ixabepilone SDF
Smiles CC1CCCC2(C(O2)CC(NC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (197.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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