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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Ixabepilone (formerly known as azaepothilone B and BMS-247550; Trade name: Ixempra) is a potent and orally bioavailable microtubule-stabilizing agent for the treatment of cancer. It attaches itself to tubulin and stimulates microtubule stabilization and tubulin polymerization, which stops cells in their G2-M phase of the cell cycle and causes tumor cells to die. The lactam analogue of epothilone B, BMS-247550 (ixabepilone), demonstrated enhanced metabolic stability, strong tubulin polymerization activity, and continued efficacy against lines resistant to paclitaxel. Ixabepilone was approved by the Food and Drug Administration in 2007 for the treatment of drug-resistant/refractory metastatic or locally advanced breast cancer, based on its demonstrated efficacy in clinical trials.
| Targets |
microtubule(tubulin stabilising)
|
|---|---|
| ln Vitro |
BMS-247550 is an extremely effective cytotoxic agent that can eradicate cancer cells even at low nanomolar concentrations. It also maintains its antineoplastic properties against human cancers that are either paclitaxel-resistant or inherently insensitive[1].
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| ln Vivo |
BMS-247550 demonstrates antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumors. The results of this study indicate that BMS-247550 is more effective than paclitaxel in all five paclitaxel-resistant tumors evaluated (four in humans and one in a mouse): the clinically derived paclitaxel-resistant Pat-7 ovarian carcinoma, the tubulin-mutated A2780Tax ovarian carcinoma that is resistant to paclitaxel, the HCT116/VM46 MDR colon carcinoma, the clinically derived paclitaxel-resistant Pat-21 breast carcinoma, and the murine fibrosarcoma M5076. A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma are the three paclitaxel-sensitive human tumor xenografts against which BMS-247550 exhibits antitumor activity comparable to paclitaxel[1].
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| Enzyme Assay |
Published techniques are used to assess the potency of BMS-247550 and paclitaxel in polymerizing tubulin isolated from calf brain. In short, tubulin is added to polymerization buffer at 37°C in microcuvette wells of a Beckman apparatus along with varying concentrations of paclitaxel or BMS-247550 [0.1 M mes, 1 mM EGTA, 0.5 mM MgCl2 (pH 6.6)]. UV spectrophotometer, model number DU 7400. The final concentration of microtubule protein is set at 1.0 mg/mL, and compound concentrations are typically used at 2.5, 5.0, and 10 μM. The instrument's software program calculates the initial slopes of absorbance (A280 nM), which are measured every 10 seconds.
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| Cell Assay |
Trypsinization is used to gather HCT116 cells from cultures after they have been exposed to 7.5 nm of BMS-247550 for 1, 2, 4, 8, 16, and 24 hours. Pelletized cells are fixed at −20°C in 80% ethanol. After being stored at −20°C for the entire night, cells are rehydrated using PBS buffer and then incubated with propidium iodide (5 μg/mL) in 0.1% RNase for 15–30 minutes to stain the DNA. The FACS Calibur device is used for the acquisition of fluorescence-activated cell sorters, and Cellquest and Modfit software are used for the analysis.
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| Animal Protocol |
Human tumor xenografts（BALB/c nu/nu nude mice）
various concentrations i.v. or p.o. |
| References |
| Molecular Formula |
C27H42N2O5S
|
|---|---|
| Molecular Weight |
506.6978
|
| Exact Mass |
506.28
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| Elemental Analysis |
C, 64.00; H, 8.35; N, 5.53; O, 15.79; S, 6.33
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| CAS # |
219989-84-1
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| Related CAS # |
219989-84-1
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| Appearance |
white solid powder
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| SMILES |
C[C@H]1CCC[C@@]2([C@@H](O2)C[C@H](NC(=O)C[C@@H](C(C(=O)[C@@H]([C@H]1O)C)(C)C)O)/C(=C/C3=CSC(=N3)C)/C)C
|
| InChi Key |
FABUFPQFXZVHFB-PVYNADRNSA-N
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| InChi Code |
InChI=1S/C27H42N2O5S/c1-15-9-8-10-27(7)22(34-27)12-20(16(2)11-19-14-35-18(4)28-19)29-23(31)13-21(30)26(5,6)25(33)17(3)24(15)32/h11,14-15,17,20-22,24,30,32H,8-10,12-13H2,1-7H3,(H,29,31)/b16-11+/t15-,17+,20-,21-,22-,24-,27+/m0/s1
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| Chemical Name |
(1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione
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| Synonyms |
Azaepothilone B; BMS 2475501; BMS247550; BMS-247550; BMS 247550
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 83.3~100 mg/mL (164.5~197.4 mM)
Ethanol: ~47 mg/mL (~92.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+30% PEG 300+2% Tween 80+ddH2O: 7mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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