Glycyl-Exatecan TFA
Based on 1 Customer Validation
Glycyl-Exatecan TFA (G-DX-8951 TFA) is a Topoisomerase I inhibitor. Glycyl-Exatecan TFA exhibits weaker in vitro cytotoxicity than DX-8951 (HY-13631), and can further release DX-8951 in vivo. Glycyl-Exatecan TFA can be used in studies related to Exatecan metabolism and antitumor drug delivery.
For research use only. We do not sell to patients.
- Purity : 98.73%
- CAS No.: 1883333-57-0
- Formula: C28H26F4N4O7
- Molecular Weight:606.52
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
All Topoisomerase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase I |
In Vitro
Glycyl-Exatecan TFA (G-DX-8951 TFA) exhibits almost comparable Topoisomerase I inhibitory activity to DX-8951 in preclinical in vitro studies, while its in vitro cytotoxicity is weaker than that of DX-8951[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (5-week-old; Meth A fibrosarcoma cells subcutaneously transplanted)[2]
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Dosage:6 mg/kg
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Administration:i.v.; single dose
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Result:Reached maximum concentrations at 5 min in plasma, tumor, and liver; showed a tissue apparent terminal t1/2 of 3.7-11 h and released DX-8951.
Chemical Information
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CAS No. 1883333-57-0
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Appearance Solid
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Molecular Weight 606.52
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Formula C28H26F4N4O7
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Color Light yellow to yellow
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SMILES
O=C(N[C@H]1CCC2=C3C1=C(CN4C(C(COC([C@@]5(CC)O)=O)=C5C=C46)=O)C6=NC3=CC(F)=C2C)CN.O=C(O)C(F)(F)F
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Synonyms
Glycyl-DX-8951 TFA; Exatecan analog 2 TFA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (164.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (295 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6488 mL | 8.2438 mL | 16.4875 mL | 41.2188 mL |
| 5 mM | 0.3298 mL | 1.6488 mL | 3.2975 mL | 8.2438 mL | |
| 10 mM | 0.1649 mL | 0.8244 mL | 1.6488 mL | 4.1219 mL | |
| 15 mM | 0.1099 mL | 0.5496 mL | 1.0992 mL | 2.7479 mL | |
| 20 mM | 0.0824 mL | 0.4122 mL | 0.8244 mL | 2.0609 mL | |
| 25 mM | 0.0660 mL | 0.3298 mL | 0.6595 mL | 1.6488 mL | |
| 30 mM | 0.0550 mL | 0.2748 mL | 0.5496 mL | 1.3740 mL | |
| 40 mM | 0.0412 mL | 0.2061 mL | 0.4122 mL | 1.0305 mL | |
| 50 mM | 0.0330 mL | 0.1649 mL | 0.3298 mL | 0.8244 mL | |
| 60 mM | 0.0275 mL | 0.1374 mL | 0.2748 mL | 0.6870 mL | |
| 80 mM | 0.0206 mL | 0.1030 mL | 0.2061 mL | 0.5152 mL | |
| 100 mM | 0.0165 mL | 0.0824 mL | 0.1649 mL | 0.4122 mL |