(4-NH2)-Exatecan
Based on 1 Customer Validation
(4-NH2)-Exatecan (compound A), a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 2495742-21-5
- Formula: C23H21N3O4
- Molecular Weight:403.43
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Topoisomerase Isoforms
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Biological Activity
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Camptothecins |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HOC-21 cell line | IC50 |
35.89 ng/mL
Compound: 34
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In vitro antitumor activity against HOC-21 (human ovarian cancer) cells.
In vitro antitumor activity against HOC-21 (human ovarian cancer) cells.
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[PMID: 9632364] |
| P388 | IC50 |
2.97 ng/mL
Compound: 34
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In vitro antitumor activity against P388 (murine leukemia) cells.
In vitro antitumor activity against P388 (murine leukemia) cells.
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[PMID: 9632364] |
| QG-56 | IC50 |
1.38 ng/mL
Compound: 34
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In vitro antitumor activity against QG-56 (human lung cancer) cells.
In vitro antitumor activity against QG-56 (human lung cancer) cells.
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[PMID: 9632364] |
(4-NH2)-Exatecan contains a linker for connecting to a Ligand Unit, wherein the linker is attached in a cleavable manner to the amino residue, characterized by the addition of an amino (NH2) functional group at the 4th position of the parent molecule[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. 2495742-21-5
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Appearance Solid
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Molecular Weight 403.43
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Formula C23H21N3O4
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Color Light yellow to yellow
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SMILES
O=C1N2C(C(C(C2)=C3C4=C5CCC3)=NC4=CC=C5N)=CC6=C1COC([C@]6(O)CC)=O
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Synonyms
AZ14170132
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (247.87 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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: 2.5 mg/mL (6.20 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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.
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 (sealed storage, away from moisture and light)
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 (275 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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 (sealed storage, away from moisture and light). 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 | 2.4787 mL | 12.3937 mL | 24.7874 mL | 61.9686 mL |
| 5 mM | 0.4957 mL | 2.4787 mL | 4.9575 mL | 12.3937 mL | |
| 10 mM | 0.2479 mL | 1.2394 mL | 2.4787 mL | 6.1969 mL | |
| 15 mM | 0.1652 mL | 0.8262 mL | 1.6525 mL | 4.1312 mL | |
| 20 mM | 0.1239 mL | 0.6197 mL | 1.2394 mL | 3.0984 mL | |
| 25 mM | 0.0991 mL | 0.4957 mL | 0.9915 mL | 2.4787 mL | |
| 30 mM | 0.0826 mL | 0.4131 mL | 0.8262 mL | 2.0656 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6197 mL | 1.5492 mL | |
| 50 mM | 0.0496 mL | 0.2479 mL | 0.4957 mL | 1.2394 mL | |
| 60 mM | 0.0413 mL | 0.2066 mL | 0.4131 mL | 1.0328 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7746 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2479 mL | 0.6197 mL |
(4-NH2)-Exatecan Related Classifications
HY-145397 Related Classifications
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