Cathepsin L-IN-2
Based on 1 publication(s) in Google Scholar
Cathepsin L-IN-2 ((Rac)-Z-Phe-Phe-FMK) is a Cathepsin L (CTSL) inhibitor. Cathepsin L-IN-2 inhibits CTSL enzymatic activity, supporting the mechanism by which CTSL mediates T-DXd linker cleavage and payload release. Cathepsin L-IN-2 is used in studies on Cathepsin L-dependent ADC payload release and breast cancer-related mechanisms.
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- Reinheit : 98.02%
- CAS. Nr.: 108005-94-3
- Formel: C27H27FN2O4
- Molecular Weight:462.51
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Speicherung:
-20°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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Cathepsin L-IN-2
MoreAlle Cathepsin Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
cathepsin L |
In Vitro
Cathepsin L-IN-2 ((Rac)-Z-Phe-Phe-FMK) (3 μM; pretreatment before T-DXd (HY-138298A) addition; 5 days or until control cells reach appropriate confluence) significantly attenuates the cytotoxicity of T-DXd in Au565 cells, increasing the IC50 of T-DXd from 27.4 ng/mL to 896 ng/mL, supporting the involvement of CTSL in T-DXd linker cleavage and payload release[1].
Cathepsin L-IN-2 (3 μM; pretreatment before T-DM1 (HY-P9921) addition; 5 days or until control cells reach appropriate confluence) has little effect on the cytotoxicity of T-DM1 in Au565 cells, with the IC50 of T-DM1 changing from 3.6 ng/mL to 4.3 ng/mL, indicating that this result is related to the CTSL-cleavable T-DXd linker[1].
Cathepsin L-IN-2 (12 μM; pH 6.0) reduces CTSL enzymatic activity derived from MDA-MB-231 cell-conditioned medium, including the elevated Z-Leu-Arg-AMC substrate cleavage activity under CTSL overexpression conditions[1].
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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CAS. Nr. 108005-94-3
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Appearance Solid
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Molecular Weight 462.51
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Formel C27H27FN2O4
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Color White to off-white
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SMILES
O=C(OCC1=CC=CC=C1)NC(CC2=CC=CC=C2)C(NC(CC3=CC=CC=C3)C(CF)=O)=O
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Synonyms
(Rac)-Z-Phe-Phe-FMK
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°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)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Effective extracellular payload release and immunomodulatory interactions govern the therapeutic effect of trastuzumab deruxtecan (T-DXd). [Abstract]2025 Apr 2;16(1):3167. PMID: 40175391
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 42.5 mg/mL (91.89 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.7 mg/mL (3.68 mM); Clear solution
This protocol yields a clear solution of ≥ 1.7 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.0 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: 1.7 mg/mL (3.68 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.7 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 (17.0 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. * 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.
Protokoll
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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.
Reinheit & Dokumentation
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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)
Verweise
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 |
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| DMSO | 1 mM | 2.1621 mL | 10.8106 mL | 21.6212 mL | 54.0529 mL |
| 5 mM | 0.4324 mL | 2.1621 mL | 4.3242 mL | 10.8106 mL | |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1621 mL | 5.4053 mL | |
| 15 mM | 0.1441 mL | 0.7207 mL | 1.4414 mL | 3.6035 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0811 mL | 2.7026 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1621 mL | |
| 30 mM | 0.0721 mL | 0.3604 mL | 0.7207 mL | 1.8018 mL | |
| 40 mM | 0.0541 mL | 0.2703 mL | 0.5405 mL | 1.3513 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3604 mL | 0.9009 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2703 mL | 0.6757 mL |
Cathepsin L-IN-2 Related Classifications
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