Tesirine
Based on 7 publication(s) in Google Scholar
Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity.
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- Pureza: 98.31%
- No. CAS: 1595275-62-9
- Fòrmula: C75H101N9O23
- Peso molecular:1496.65
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Almacenamiento:
-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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tesirine
More- Nature. 2024 Apr;628(8007):416-423. [Abstract]
- Nat Cancer. 2025 Dec;6(12):2011-2024. [Abstract]
- Cell Rep. 2023 Nov 28;42(12):113503. [Abstract]
- Mol Cancer Ther. 2026 Jan 10:10.1158/1535-7163.MCT-25-0450. [Abstract]
- Med Drug Discov. 2025 Sep 20;28:100226.
- bioRxiv. 2025 Aug 21:2025.08.17.670714. [Abstract]
- bioRxiv. 2024 Sep 25:2024.09.23.614576. [Abstract]
Ver todos los productos específicos de isoformas Drug-Linker Conjugates for ADC
More
Actividad biológica
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Pyrrolobenzodiazepines |
Tesirine (SG3199) is the released warhead component of the ADC payload Tesirine. Tesirine inhibits K562, NCIN87, BT474, and SKBR3 cancer cells with IC50s of 150 pM, 20 pM, 1 nM and 320 pM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1595275-62-9
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Appearance Solid
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Peso molecular 1496.65
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Fòrmula C75H101N9O23
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Color White to light yellow
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SMILES
O=C(NC1=CC=C(COC(N2[C@@H](O)[C@@](CC(C)=C3)([H])N3C(C4=CC(OC)=C(OCCCCCOC5=C(OC)C=C6C(N7[C@](CC(C)=C7)([H])C=NC6=C5)=O)C=C42)=O)=O)C=C1)[C@H](C)NC([C@H](C(C)C)NC(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCN8C(C=CC8=O)=O)=O)=O)=O
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Synonyms
SG3249
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-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 (7)
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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 -
Nat Cancer
2025 Dec;6(12):2011-2024. PMID: 41429932 -
Cell Rep
Engineering CD276/B7-H3-targeted antibody-drug conjugates with enhanced cancer-eradicating capability. [Abstract]2023 Nov 28;42(12):113503. PMID: 38019654 -
Mol Cancer Ther
Identification of CADM1 as an Immunotherapeutic Target and Evaluation of a Novel CADM1-Targeting Antibody-Drug Conjugate in Preclinical Osteosarcoma Models. [Abstract]2026 Jan 10:10.1158/1535-7163.MCT-25-0450. PMID: 41517891 -
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bioRxiv
2025 Aug 21:2025.08.17.670714. PMID: 40894621 -
bioRxiv
2024 Sep 25:2024.09.23.614576. PMID: 39386470
Solvente y solubilidad
DMSO : 200 mg/mL (133.63 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: ≥ 5 mg/mL (3.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (278 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tiberghien AC, et al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016;7(11):983-987. Published 2016 May 24. [Content Brief]
[2]. Hartley JA, 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;8(1):10479. Published 2018 Jul 11. [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 | 0.6682 mL | 3.3408 mL | 6.6816 mL | 16.7040 mL |
| 5 mM | 0.1336 mL | 0.6682 mL | 1.3363 mL | 3.3408 mL | |
| 10 mM | 0.0668 mL | 0.3341 mL | 0.6682 mL | 1.6704 mL | |
| 15 mM | 0.0445 mL | 0.2227 mL | 0.4454 mL | 1.1136 mL | |
| 20 mM | 0.0334 mL | 0.1670 mL | 0.3341 mL | 0.8352 mL | |
| 25 mM | 0.0267 mL | 0.1336 mL | 0.2673 mL | 0.6682 mL | |
| 30 mM | 0.0223 mL | 0.1114 mL | 0.2227 mL | 0.5568 mL | |
| 40 mM | 0.0167 mL | 0.0835 mL | 0.1670 mL | 0.4176 mL | |
| 50 mM | 0.0134 mL | 0.0668 mL | 0.1336 mL | 0.3341 mL | |
| 60 mM | 0.0111 mL | 0.0557 mL | 0.1114 mL | 0.2784 mL | |
| 80 mM | 0.0084 mL | 0.0418 mL | 0.0835 mL | 0.2088 mL | |
| 100 mM | 0.0067 mL | 0.0334 mL | 0.0668 mL | 0.1670 mL |
Tesirine Related Classifications
HY-128952 Related Classifications
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