SG3199
Based on 3 publication(s) in Google Scholar
SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).
For research use only. We do not sell to patients.
- Purity: 98.33%
- CAS No.: 1595275-71-0
- Formula: C33H36N4O6
- Molecular Weight:584.66
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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)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SG3199
More
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Biological Activity
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Pyrrolobenzodiazepines |
SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines with a mean GI50 of 151.5 pM. Cells defective in DNA repair protein ERCC1 or homologous recombination repair show increased sensitivity to SG3199 and the drug is only moderately susceptible to multidrug resistance mechanisms[1].
SG3199 is highly efficient at producing DNA interstrand cross-links in naked linear plasmid DNA and dose-dependent cross-linking is observed in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Following i.v. administration at 0.1 μg/kg, 0.5 μg/kg and 1 μg/kg, SG3199 shows a very rapid clearance in rats. In the 0.5 μg/kg and 1 μg/kg dose groups, the rapid clearance was between 1000 and 1500 mL/h/kg, with a T1/2 between 8 and 42 minutes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1595275-71-0
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Appearance Solid
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Molecular Weight 584.66
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Formula C33H36N4O6
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Color White to off-white
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SMILES
O=C1N2[C@](CC(C)=C2)([H])C=NC3=CC(OCCCCCOC4=C(OC)C=C5C(N6[C@](CC(C)=C6)([H])C=NC5=C4)=O)=C(OC)C=C13
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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)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2024 Apr;628(8007):416-423. PMID: 38538786
SG3199 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Apr;628(8007):416-423. [Abstract]
Jurkat cells or Jurkat TCR-KO cells were treated with anti-TRBC1 antibodies, anti-TRBC1–SG3249 ADC or SG3199 free drug at the indicated concentration. Cell growth was quantified as green calibrated unit (GCU) using live-cell imaging.
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Mol Pharm
Identification of 5-Carboxyfluorescein as a Probe Substrate of SLC46A3 and Its Application in a Fluorescence-Based In Vitro Assay Evaluating the Interaction with SLC46A3. [Abstract]2023 Jan 2;20(1):491-499. PMID: 36458938
SG3199 purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2023 Jan 2;20(1):491-499. [Abstract]
Both DM1 and SG3199 (0.1-200 μM; 5 min) inhibits SLC46A3 dC-mediated 5-CF (1 μM) uptake in a concentration-dependent manner, with the IC50s of 16.4 and 43.6 μM, respectively, in MDCKII/SLC46A3 dC cells.
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Bioorg Med Chem Lett
2019 Feb 15;29(4):549-555. PMID: 30630717
Solvent & Solubility
DMSO : 130 mg/mL (222.35 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 (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)
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: ≥ 3.25 mg/mL (5.56 mM); Clear solution
This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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.
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 (protect from light, 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.
Purity & Documentation
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Data Sheet (274 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
[1]. John A Hartley, et al. Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine. Sci Rep. 2018 Jul 11;8(1):10479. [Content Brief]
[2]. Francesca Zammarchi, et al. ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood. 2018 Mar 8;131(10):1094-1105. [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, 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 | 1.7104 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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