| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Epothilone A (also abbreviated as Epo A), similar to paclitaxel in terms of mechanism of action, is also a naturally occurring microtubule-stabilizing macrolide agent (also called mitotic inhibitor or tubulin inhibitor) isolated from the myxobacterium Sorangium cellulosum with potential antineoplastic activity. It acts by inhibiting the polymerization of tubulin. The antiproliferative IC50 value of Epothilone A in HCT-116 cell line is 4.4 nM. It has been found that the SKOV-3 human ovarian cancer cells were susceptible to Epothilone A with IC50 value of 20.4 ± 1.4 nM. The antiproliferative capacity of Epothilone A in SKOV-3 cell line (measured as IC50 after 72 h continuous treatment) was six times greater than that of PTX’s. Besides, Epothilone A induced time coursedependent apoptosis and necrosis.
| ln Vitro |
Epothilone A is a competitive inhibitor that prevents tubulin polymers from binding to [3H] paclitaxel. According to Hanes and Dixon analyses, Epothilone A's apparent Ki value is 1.4 μM and 0.6 μM, respectively[1]. When epothilone A is applied to the human T-24 bladder carcinoma cell line in vitro, it is observed to be highly cytotoxic (IC50=0.05 μM). Based on competition experiments, the binding affinities of paclitaxel and epothilone A to tubulin are of the same order of magnitude. The inhibitory concentration (IC50) of paclitaxel (3.6 μM), epothilone A (2.3 μM), and patupilone (3.3 μM) required to remove 100 nM of (3H) paclitaxel from the tubulin binding site[2].
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| ADME/Pharmacokinetics |
Metabolism / Metabolites
PBBs can be absorbed via oral, inhalation, and dermal routes. Due to their lipophilic nature, PBBs, especially the highly brominated congeners, tend to accumulate in lipid-rich tissues such as the liver, adipose, skin, and breast milk. Certain PBB compounds are metabolized by the microsomal monooxygenase system catalyzed by cytochrome P-450 of the type induced by phenobarbital. The rate of metabolism may depends on the bromine substitution pattern. PBB congeners of low bromine content are transformed into hydroxylated derivatives that are predominately eliminated in the urine. Highly brominated congeners are either retained or excreted unchanged in the feces. (L628) |
||
| References | |||
| Additional Infomation |
Epothilone A is an epithilone that is epothilone C in which the double bond in the macrocyclic lactone ring has been oxidised to the corresponding epoxide (the 13R,14S diastereoisomer). It has a role as an antineoplastic agent, a tubulin modulator, a metabolite and a microtubule-stabilising agent. It is an epoxide and an epothilone.
Epothilone A has been reported in Brassica napus and Sorangium cellulosum with data available. Epothilone A is an extract from the myxobacteria Sorangium cellulosum that promotes tubulin polymerization and microtubule stabilization, thereby inhibiting mitosis. Epothilone A appears to be less potent than Epothilone B. (NCI) 2-Monobromobiphenyl is a polybrominated biphenyl. Polybrominated biphenyls (PBBs) are a group of 209 synthetic organic compounds with 1-10 bromine atoms attached to biphenyl. They can be used as flame retardants and may be added to the plastics used to make products like computer monitors, televisions, textiles, and plastic foams to make them difficult to burn. However, the use of PBBs is banned or restricted in most areas due to their toxicity and persistence in the environment. (L628, L629) |
| Molecular Formula |
C26H39NO6S
|
|
|---|---|---|
| Molecular Weight |
493.66
|
|
| Exact Mass |
493.249
|
|
| CAS # |
152044-53-6
|
|
| Related CAS # |
|
|
| PubChem CID |
448799
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.1±0.1 g/cm3
|
|
| Boiling Point |
683.3±55.0 °C at 760 mmHg
|
|
| Melting Point |
95ºC
|
|
| Flash Point |
367.1±31.5 °C
|
|
| Vapour Pressure |
0.0±2.2 mmHg at 25°C
|
|
| Index of Refraction |
1.532
|
|
| LogP |
2.54
|
|
| Hydrogen Bond Donor Count |
2
|
|
| Hydrogen Bond Acceptor Count |
8
|
|
| Rotatable Bond Count |
2
|
|
| Heavy Atom Count |
34
|
|
| Complexity |
770
|
|
| Defined Atom Stereocenter Count |
7
|
|
| SMILES |
C[C@H]1CCC[C@@H]2[C@@H](O2)C[C@H](OC(=O)C[C@@H](C(C(=O)[C@@H]([C@H]1O)C)(C)C)O)/C(=C/C3=CSC(=N3)C)/C
|
|
| InChi Key |
HESCAJZNRMSMJG-KKQRBIROSA-N
|
|
| InChi Code |
InChI=1S/C26H39NO6S/c1-14-8-7-9-19-21(32-19)11-20(15(2)10-18-13-34-17(4)27-18)33-23(29)12-22(28)26(5,6)25(31)16(3)24(14)30/h10,13-14,16,19-22,24,28,30H,7-9,11-12H2,1-6H3/b15-10+/t14-,16+,19+,20-,21-,22-,24-/m0/s1
|
|
| Chemical Name |
(1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12-tetramethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.21 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 (4.21 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 (4.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0257 mL | 10.1284 mL | 20.2569 mL | |
| 5 mM | 0.4051 mL | 2.0257 mL | 4.0514 mL | |
| 10 mM | 0.2026 mL | 1.0128 mL | 2.0257 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA