Rezetecan
Based on 1 Customer Validation
Rezetecan is a topoisomerase I inhibitor with cytotoxicity. Rezetecan can serve as an antibody-drug conjugate payload (ADC Payloads), for example, it participates in the synthesis of Tizetatug rezetecan (HY-177711). Rezetecan is applicable to research related to various cancers such as breast cancer and gastric cancer.
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- Purity : 98.90%
- 화학식: C58H67FN10O15S
- 분자량:1195.27
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All Topoisomerase Isoforms
More
Biological Activity
제품 설명
In Vitro
Rezetecan (SHR9265) (0.1-400 nmol/L; 6 days) potently inhibits the growth of human prostate cancer cell lines C4-2, DU145, PC3, 22RV1 and LNCaP in vitro, with IC50 values ranging from 2.41 to 7.74 nM[2].
Rezetecan serves as the toxic payload of Tizetatug rezetecan (HY-177711). Tizetatug rezetecan exhibits anti-tumor activity, blocks the repair of topoisomerase I-induced single-strand breaks to trigger DNA double-strand breaks, and induces DNA damage and apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Appearance Solid
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분자량 1195.27
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화학식 C58H67FN10O15S
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Color White to off-white
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SMILES
O=C(O)[C@@H](N)CSC(C1)C(N(CCCCCC(NCC(NCC(N[C@@H](CC2=CC=CC=C2)C(NCC(NCO[C@H](C3CC3)C(N[C@H]4CCC5=C6C4=C(CN7C(C(COC([C@@]8(CC)O)=O)=C8C=C79)=O)C9=NC6=CC(F)=C5C)=O)=O)=O)=O)=O)=O)C1=O)=O
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Synonyms
SHR9265
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (83.66 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. 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. 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.09 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 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.
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.
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
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Data Sheet (275 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. 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 |
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| DMSO | 1 mM | 0.8366 mL | 4.1832 mL | 8.3663 mL | 20.9158 mL |
| 5 mM | 0.1673 mL | 0.8366 mL | 1.6733 mL | 4.1832 mL | |
| 10 mM | 0.0837 mL | 0.4183 mL | 0.8366 mL | 2.0916 mL | |
| 15 mM | 0.0558 mL | 0.2789 mL | 0.5578 mL | 1.3944 mL | |
| 20 mM | 0.0418 mL | 0.2092 mL | 0.4183 mL | 1.0458 mL | |
| 25 mM | 0.0335 mL | 0.1673 mL | 0.3347 mL | 0.8366 mL | |
| 30 mM | 0.0279 mL | 0.1394 mL | 0.2789 mL | 0.6972 mL | |
| 40 mM | 0.0209 mL | 0.1046 mL | 0.2092 mL | 0.5229 mL | |
| 50 mM | 0.0167 mL | 0.0837 mL | 0.1673 mL | 0.4183 mL | |
| 60 mM | 0.0139 mL | 0.0697 mL | 0.1394 mL | 0.3486 mL | |
| 80 mM | 0.0105 mL | 0.0523 mL | 0.1046 mL | 0.2614 mL |
Rezetecan Related Classifications
HY-147408 Related Classifications
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