SG2057
Based on 1 Customer Validation
SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.
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- Pureté : 99.93%
- CAS No.: 260417-62-7
- Formule: C33H36N4O6
- Masse moléculaire:584.66
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Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Pyrrolobenzodiazepines |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
<0.001 μM
Compound: 4b
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Inhibitory concentration against human K562 leukemia cells following incubation for 1 hour
Inhibitory concentration against human K562 leukemia cells following incubation for 1 hour
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[PMID: 14971896] |
| NCI-H460 | IC50 |
0.062 nM
Compound: 3
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Cytotoxicity against human NCI-H460 cells after 24 hrs under hypoxic condition by luminescence-based Cell-Titer Glo assay
Cytotoxicity against human NCI-H460 cells after 24 hrs under hypoxic condition by luminescence-based Cell-Titer Glo assay
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[PMID: 29079474] |
| NCI-H460 | IC50 |
0.092 nM
Compound: 3
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Cytotoxicity against human NCI-H460 cells after 24 hrs under normoxic condition by luminescence-based Cell-Titer Glo assay
Cytotoxicity against human NCI-H460 cells after 24 hrs under normoxic condition by luminescence-based Cell-Titer Glo assay
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[PMID: 29079474] |
In Vitro
SG2057 has multilog differential in vitro cytotoxicity against a panel of human tumour cell lines with a mean GI50 of 212 pM. SG2057 is highly efficient at producing DNA interstrand cross-links in cells which form rapidly and persist over a 48 h period[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:Female NCr-nude mice injected with SKOV-3 cells[1]
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Dosage:5 μg/kg, 10 μg/kg, 20 μg/kg, 30 μg/kg, 40 μg/kg, 50 μg/kg, 60 μg/kg
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Administration:i.v.; daily, once a week, or once every four days
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Result:Showed significant antitumor activity.
Chemical Information
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CAS No. 260417-62-7
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Appearance Solid
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Masse moléculaire 584.66
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Formule C33H36N4O6
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Color White to light yellow
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SMILES
O=C1N2[C@](CC(C2)=C)([H])C=NC3=CC(OCCCCCOC4=C(OC)C=C5C(N6[C@](CC(C6)=C)([H])C=NC5=C4)=O)=C(OC)C=C13
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Synonyms
DRG16
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (171.04 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, 6 months; -20°C, 1 month (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 (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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 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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Instruction de manipulation (2659 KB)
Références
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 (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 | 1.7104 mL | 8.5520 mL | 17.1040 mL | 42.7599 mL |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4208 mL | 8.5520 mL | |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7104 mL | 4.2760 mL | |
| 15 mM | 0.1140 mL | 0.5701 mL | 1.1403 mL | 2.8507 mL | |
| 20 mM | 0.0855 mL | 0.4276 mL | 0.8552 mL | 2.1380 mL | |
| 25 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7104 mL | |
| 30 mM | 0.0570 mL | 0.2851 mL | 0.5701 mL | 1.4253 mL | |
| 40 mM | 0.0428 mL | 0.2138 mL | 0.4276 mL | 1.0690 mL | |
| 50 mM | 0.0342 mL | 0.1710 mL | 0.3421 mL | 0.8552 mL | |
| 60 mM | 0.0285 mL | 0.1425 mL | 0.2851 mL | 0.7127 mL | |
| 80 mM | 0.0214 mL | 0.1069 mL | 0.2138 mL | 0.5345 mL | |
| 100 mM | 0.0171 mL | 0.0855 mL | 0.1710 mL | 0.4276 mL |
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