(αR)-Cyclopropaneacetamide-Exatecan
Based on 1 Customer Validation
(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 2414254-37-6
- Formula: C29H28FN3O6
- Molecular Weight:533.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
All Topoisomerase Isoforms
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Biological Activity
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Camptothecins |
SHR169265 exhibits potent, HER2 expression-independent cytotoxicity against 9 human cancer cell lines, with IC50 values ranging from 0.30 nM to 2.32 nM after 6 days of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-N87, SK-BR-3, HCC1954, JIMT-1, Capan-1, AGS, MKN45, SNU-16, MDA-MB-468
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Concentration:Serially diluted concentrations
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Incubation Time:6 days
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Result:Induced strong cytotoxicity across all tested cell lines, with IC50 values of 1.00±0.07 nM (NCI-N87), 0.58±0.10 nM (SK-BR-3), 0.55±0.19 nM (HCC1954), 2.32±0.45 nM (JIMT-1), 0.38±0.07 nM (Capan-1), 0.36±0.11 nM (AGS), 0.30±0.07 nM (MKN45), 0.57±0.19 nM (SNU-16), and 0.56±0.09 nM (MDA-MB-468).
| Species | Dose | Route | Cmax | AUC0-t | T1/2 | CL | Vss |
|---|---|---|---|---|---|---|---|
| Mice[1] | 0.5 mg/kg | i.v. | 250 ng/mL | 113 ng·h/mL | 0.37 h | 72.6 mL/min/kg | 1815 mL/kg |
SHR-A1811 (1-10 mg/kg; i.p.; single dose; once weekly for 2 doses), delivering target reagent SHR169265, induces dose-dependent tumor growth inhibition (57.9% to 108.8% TGI) in HER2-moderate breast cancer xenografts, with repeated dosing enhancing efficacy[1].
SHR-A1811 (1-6 mg/kg; i.p.; single dose), delivering target reagent SHR169265, induces dose-dependent tumor growth inhibition (91% to 120% TGI) in HER2-low pancreatic cancer xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NU/NU nude mice with Gastric cancer (female, 15-18g); Beige SCID mice (female, 15-18g); Balb/c nude mice (female, 15-18g)[1]
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Dosage:1 mg/kg; 3 mg/kg; 6 mg/kg
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Administration:i.p.; single dose
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Result:Induced 85% TGI at 1 mg/kg.
Induced 124% TGI with sustained tumor regression through day 17 at 3 mg/kg.
Induced 119% TGI with sustained tumor regression through day 17 at 6 mg/kg.
Maintained low and stable tumoral levels at 1 mg/kg.
Reached tumoral Cmax at 24 hours at 3 mg/kg.
Reached tumoral Cmax at 72 hours at 6 mg/kg.
Induced PARP cleavage in tumor cells, with degree correlated with tumoral SHR169265 levels.
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Animal Model:NU/NU nude mice with Breast cancer (female, 15-18g); Beige SCID mice (female, 15-18g); Balb/c nude mice (female, 15-18g)[1]
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Dosage:5 mg/kg (single dose); 10 mg/kg (single dose); 1 mg/kg (weekly x2); 3 mg/kg (weekly x2); 6 mg/kg (weekly x2)
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Administration:i.p.; single dose; once weekly for 2 doses
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Result:Induced 57.9% TGI at 5 mg/kg single dose.
Induced 80.7% TGI at 10 mg/kg single dose.
Induced 91.8% TGI at 1 mg/kg once weekly for 2 doses.
Induced 108.8% TGI at 3 mg/kg once weekly for 2 doses.
Induced 101.4% TGI at 6 mg/kg once weekly for 2 doses.
Chemical Information
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CAS No. 2414254-37-6
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Appearance Solid
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Molecular Weight 533.55
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Formula C29H28FN3O6
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Color Light yellow to yellow
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SMILES
O[C@H](C1CC1)C(N[C@@H]2C3=C4C(C(N5C4)=CC([C@](O)(C(OC6)=O)CC)=C6C5=O)=NC7=CC(F)=C(C)C(CC2)=C73)=O
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Synonyms
SHR169265
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (187.42 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)
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.
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.
Purity & Documentation
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Data Sheet (287 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)
- 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8742 mL | 9.3712 mL | 18.7424 mL | 46.8560 mL |
| 5 mM | 0.3748 mL | 1.8742 mL | 3.7485 mL | 9.3712 mL | |
| 10 mM | 0.1874 mL | 0.9371 mL | 1.8742 mL | 4.6856 mL | |
| 15 mM | 0.1249 mL | 0.6247 mL | 1.2495 mL | 3.1237 mL | |
| 20 mM | 0.0937 mL | 0.4686 mL | 0.9371 mL | 2.3428 mL | |
| 25 mM | 0.0750 mL | 0.3748 mL | 0.7497 mL | 1.8742 mL | |
| 30 mM | 0.0625 mL | 0.3124 mL | 0.6247 mL | 1.5619 mL | |
| 40 mM | 0.0469 mL | 0.2343 mL | 0.4686 mL | 1.1714 mL | |
| 50 mM | 0.0375 mL | 0.1874 mL | 0.3748 mL | 0.9371 mL | |
| 60 mM | 0.0312 mL | 0.1562 mL | 0.3124 mL | 0.7809 mL | |
| 80 mM | 0.0234 mL | 0.1171 mL | 0.2343 mL | 0.5857 mL | |
| 100 mM | 0.0187 mL | 0.0937 mL | 0.1874 mL | 0.4686 mL |
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