7-Epi-docetaxel
Based on 1 Customer Validation
7-Epi-docetaxel (4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere) is the major C7 epimeric impurity/in vivo metabolite of Docetaxel (HY-B0011). 7-Epi-docetaxel acts as a potent allosteric activator of rhCYP1B1. 7-Epi-docetaxel exhibits certain cell line-specific anti-migratory activity. 7-Epi-docetaxel can be used in research related to melanoma and lung adenocarcinoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.76%
- CAS. Nr.: 153381-68-1
- Formel: C43H53NO14
- Molecular Weight:807.88
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CYP1B1 |
In Vitro
7-Epi-docetaxel (3-100 μM) potently activates recombinant human CYP1B1-mediated EROD activity: the activity increases by more than 7-fold at 10 μM, 4.8-fold at 30 μM, and 4.7-fold at 100 μM, while no significant effect is observed at 3 μM[1].
7-Epi-docetaxel (1 μM) is not metabolized in vitro by recombinant human CYP1B1 expressed in insect cell Supersomes[1].
7-Epi-docetaxel (0.01-10 μM; 24-72 h) inhibits the proliferation of human lung adenocarcinoma A549 cells and mouse melanoma B16F10 cells in a concentration- and time-dependent manner, with its IC50 values ranging from 0.024 nM to 2500 nM depending on the cell line and incubation time[2].
7-Epi-docetaxel (2 nM; 24 h) exhibits 58% antimetastatic activity against human lung adenocarcinoma cell line A549 and 21% antimetastatic activity against mouse melanoma cell line B16F10[2].
7-Epi-docetaxel (2 nM; 24 h) exerts no significant effect on the activities of MMP-2 or MMP-9 in human lung adenocarcinoma cells A549 or mouse melanoma cells B16F10[2].
7-Epi-docetaxel (2-25 nM; 24-48 h) arrests human lung adenocarcinoma A549 cells at the S, G2-M and G0-G1 phases in a concentration- and time-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human lung adenocarcinoma cells, B16F10 mouse melanoma cells
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Concentration:0.01 nM, 1 μM, 10 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Exhibited an IC50 of 6.5 nM after 24 h, 0.024 nM after 48 h, and 0.112 nM after 72 h against A549 cells.
Exhibited an IC50 of 2500 nM after 24 h, 0.512 nM after 48 h, and 0.3 nM after 72 h against B16F10 cells.
Showed concentration- and time-dependent inhibition of cell proliferation.
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Cell Line:A549 human lung adenocarcinoma cells, B16F10 mouse melanoma cells
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Concentration:2 nM
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Incubation Time:24 h
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Result:Resulted in 41.92% wound coverage, corresponding to 58% anti-metastatic activity against A549 cells.
Resulted in 79.01% wound coverage, corresponding to 21% anti-metastatic activity against B16F10 cells.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:2 nM, 10 nM, 25 nM
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Incubation Time:24 h, 48 h
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Result:Caused no changes in S or G2-M phase after 24 h or 48 h treatment at 2 nM.
Caused 1.8-fold increased accumulation of cells in S phase and 2.1-fold increased accumulation in G2-M phase compared to untreated cells, plus 16% increased arrest in G0-G1 phase compared to TXT after 24 h treatment at 10 nM.
Caused increased arrest in S phase compared to 24 h treatment, no significant change in G2-M phase, and 2.41-fold increased accumulation in G0-G1 phase compared to TXT after 48 h treatment at 10 nM.
Resulted in cell cycle distribution almost similar to that at 10 nM concentration at 25 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6-8 weeks old, 18-22 g, intravenous injection of 0.1 million B16F10 melanoma cells)[2]
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Dosage:4 mg/kg
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Administration:i.v.; single dose
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Result:Showed 1.56-, 1.5-, 1.35-, and 1.12-fold increased mean group weight loss at days 2, 4, 6, and 8 post-dose respectively compared to docetaxel alone.
Did not reduce pulmonary metastatic colony formation relative to untreated control and docetaxel-only groups.
Chemical Information
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CAS. Nr. 153381-68-1
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Appearance Solid
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Molecular Weight 807.88
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Formel C43H53NO14
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Color White to light yellow
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SMILES
CC(O[C@@]1([C@](C[C@H]2O)([H])OC1)[C@@]([C@@]2(C3=O)C)([H])[C@@H]([C@@](C4(C)C)(C[C@H](OC([C@H](O)[C@H](C5=CC=CC=C5)NC(OC(C)(C)C)=O)=O)C(C)=C4[C@H]3O)O)OC(C6=CC=CC=C6)=O)=O
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Synonyms
4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (123.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Bournique B, et al. Docetaxel (Taxotere) is not metabolized by recombinant human CYP1B1 in vitro, but acts as an effector of this isozyme. Drug Metab Dispos. 2002;30(11):1149-1152. [Content Brief]
[2]. Manjappa AS, et al. Unravelling the anticancer efficacy of 10-oxo-7-epidocetaxel: in vitro and in vivo results. Drug Dev Ind Pharm. 2019;45(3):474-484. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.2378 mL | 6.1890 mL | 12.3781 mL | 30.9452 mL |
| 5 mM | 0.2476 mL | 1.2378 mL | 2.4756 mL | 6.1890 mL | |
| 10 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL | 3.0945 mL | |
| 15 mM | 0.0825 mL | 0.4126 mL | 0.8252 mL | 2.0630 mL | |
| 20 mM | 0.0619 mL | 0.3095 mL | 0.6189 mL | 1.5473 mL | |
| 25 mM | 0.0495 mL | 0.2476 mL | 0.4951 mL | 1.2378 mL | |
| 30 mM | 0.0413 mL | 0.2063 mL | 0.4126 mL | 1.0315 mL | |
| 40 mM | 0.0309 mL | 0.1547 mL | 0.3095 mL | 0.7736 mL | |
| 50 mM | 0.0248 mL | 0.1238 mL | 0.2476 mL | 0.6189 mL | |
| 60 mM | 0.0206 mL | 0.1032 mL | 0.2063 mL | 0.5158 mL | |
| 80 mM | 0.0155 mL | 0.0774 mL | 0.1547 mL | 0.3868 mL | |
| 100 mM | 0.0124 mL | 0.0619 mL | 0.1238 mL | 0.3095 mL |
7-Epi-docetaxel Related Classifications
HY-16676 Related Classifications
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