Ixabepilone Microtubule Associated inhibitor

Cat.No.S7930

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 Microtubule Associated inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 506.70

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 506.70 Formula

C27H42N2O5S

Storage (From the date of receipt)
CAS No. 219989-84-1 Download SDF Storage of Stock Solutions

Synonyms Azaepothilone B, BMS-247550, Aza-epothilone B Smiles CC1CCCC2(C(O2)CC(NC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (197.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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].

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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