Ixabepilone (BMS-247550)

Catalog No.S7930 Synonyms: Azaepothilone B, BMS 247550, BMS 247550-1, Ixempra

Ixabepilone (BMS-247550) Chemical Structure

Molecular Weight(MW): 506.70

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.

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Choose Selective Microtubule Associated Inhibitors

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

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 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].

Protocol

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Human tumor xenografts(BALB/c nu/nu nude mice)
  • Formulation: (a) ethanol:water (1:9, v/v), (b) Cremophor:ethanol:water (1:1:8, v/v) or (c)0.25 M sodium phosphate buffer (pH 8.0) at a ratio of 30:70, v/v.
  • Dosages: various concentrations
  • Administration: i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (197.35 mM)
Ethanol 100 mg/mL (197.35 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
7mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 506.70
Formula

C27H42N2O5S

CAS No. 219989-84-1
Storage powder
in solvent
Synonyms Azaepothilone B, BMS 247550, BMS 247550-1, Ixempra

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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.

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Microtubule Associated Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID