LLC355
Based on 1 Customer Validation
LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader with a DC50 of 150.8 nM. LLC355 induces DDR1 protein degradation via lysosome-mediated autophagy. LLC355 inhibits the tumorigenicity, migration and invasion abilities of cancer cells, and induces apoptosis. LLC355 is applicable to research related to non-small cell lung cancer and pancreatic cancer.
(Pink: DDR1 Target protein ligand; Blue: LC3 ligand (HY-50759); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.71%
- Formula: C63H64ClF3N10O5
- Molecular Weight:1133.69
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Storage:Powder -20°C, 3 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
Biological Activity
Compound LLC355 (0.3-10000 nM; 1-24 h) dose- and time-dependently degrades DDR1 protein in NCI-H23 cells with a DC50 of 150.8 nM, without altering DDR2 levels[1].
Compound LLC355 (0.3 μM; 24 h) potently inhibits migration and invasion of NCI-H23 cells and reduces N-cadherin expression[1].
Compound LLC355 (0.1-1 μM; 10 days) potently suppresses colony formation of NCI-H23 cells over 10 days, with greater potency than DDR1 inhibitor 1[1].
Compound LLC355 (100-1000 nM; 24 h) does not induce apoptosis in NCI-H23 cells at 0.3 μM after 24 h treatment, but induces apoptosis at 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H23
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Concentration:0.3 μM (24 h); 1 μM (24 h); 1-10000 nM (12 h); 1 μM (1 h, 3 h, 6 h, 12 h, 24 h)
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Incubation Time:1 h, 3 h, 6 h, 12 h, 24 h
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Result:Induced 40% DDR1 degradation at 0.3 μM after 24 h treatment.
Induced 92% DDR1 degradation at 1 μM after 24 h treatment.
Dose-dependently degraded DDR1 with a DC50 value of 150.8 nM after 12 h treatment.
Time-dependently degraded DDR1 with maximal degradation observed at 24 h when treated with 1 μM.
Did not affect DDR2 protein levels at evaluated concentrations.
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Cell Line:PANC-1, MIA-PaCa-2
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Concentration:0.3 and 1 μM
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Incubation Time:24 h
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Result:Inhibited cell migration.
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Cell Line:PANC-1, MIA-PaCa-2
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Concentration:0.3 and 1 μM
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Incubation Time:24 h
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Result:Inhibited cell invasion.
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Cell Line:PANC-1, MIA-PaCa-2
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Concentration:0.1, 0.3 and 1 μM
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Incubation Time:24 h
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Result:Down-regulated the expression of N-Cadherin protein in a concentration-dependent manner.
Induced PARP cleavage in a concentration-dependent manner (i.e., promotes cell apoptosis).
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Cell Line:NCI-H23
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Concentration:0.1, 0.3 and 1 μM
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Incubation Time:10 days
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Result:Potently suppressed colony formation in NCI-H23 cells.
Chemical Information
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Appearance Solid
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Molecular Weight 1133.69
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Formula C63H64ClF3N10O5
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Color White to light yellow
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SMILES
O=C1C2=CC=C(Cl)C=C2N=C([C@H](N(C(C3=CC=C(C)C=C3)=O)CCCNC(COCCN4CCN(CC5=CC(C(F)(F)F)=CC(NC(C6=CC(C#CC(C=N7)=CN8C7=CC=N8)=C(CC)C=C6)=O)=C5)CC4)=O)C(C)C)N1CC9=CC=CC=C9
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (88.21 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.21 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 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: ≥ 2.5 mg/mL (2.21 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). 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 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.
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 (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)
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 | 0.8821 mL | 4.4104 mL | 8.8208 mL | 22.0519 mL |
| 5 mM | 0.1764 mL | 0.8821 mL | 1.7642 mL | 4.4104 mL | |
| 10 mM | 0.0882 mL | 0.4410 mL | 0.8821 mL | 2.2052 mL | |
| 15 mM | 0.0588 mL | 0.2940 mL | 0.5881 mL | 1.4701 mL | |
| 20 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL | 1.1026 mL | |
| 25 mM | 0.0353 mL | 0.1764 mL | 0.3528 mL | 0.8821 mL | |
| 30 mM | 0.0294 mL | 0.1470 mL | 0.2940 mL | 0.7351 mL | |
| 40 mM | 0.0221 mL | 0.1103 mL | 0.2205 mL | 0.5513 mL | |
| 50 mM | 0.0176 mL | 0.0882 mL | 0.1764 mL | 0.4410 mL | |
| 60 mM | 0.0147 mL | 0.0735 mL | 0.1470 mL | 0.3675 mL | |
| 80 mM | 0.0110 mL | 0.0551 mL | 0.1103 mL | 0.2756 mL |
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