LDN-211904 oxalate
Based on 1 publication(s) in Google Scholar
LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC.
For research use only. We do not sell to patients.
- Purity: 99.0%
- CAS No.: 1198408-78-4
- Formula: C21H21ClN4O5
- Molecular Weight:444.87
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Publications Citing Use of MedChemExpress (MCE) LDN-211904 oxalate
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Biological Activity
IC50: 0.079 µM (EphB3)[1]
LDN-211904 (20 μM; 24 h) oxalate induces apoptosis by increasing c-PARP in SW48 resistant cells[2].
LDN-211904 (20 μM; 4-20 h) oxalate decreases the levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW48 and SW48 Cetuximab-resistant (SW48R) cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Induced apoptosis by increasing c-PARP.
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Cell Line:SW48 and SW48 Cetuximab-resistant (SW48R) cells
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Concentration:20 μM
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Incubation Time:4 h, 8 h, 20 h
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Result:The levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells were decreased.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old female BALB/c nude mice were implanted subcutaneously SW48 cells[2]
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Dosage:0.1 mg/kg
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Administration:i.p.; three times a week; for 21 days
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Result:Inhibited tumor growth.
Chemical Information
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CAS No. 1198408-78-4
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Appearance Solid
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Molecular Weight 444.87
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Formula C21H21ClN4O5
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Color White to off-white
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SMILES
O=C(C(O)=O)O.O=C(C1=CN=C2C=CC(C3CCNCC3)=CN21)NC4=C(Cl)C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (224.78 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). 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). 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 (5.62 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 (5.62 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.
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)
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 (276 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
[1]. Qiao L, et al. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6122-6. [Content Brief]
[2]. Park SH, et al. Sonic hedgehog pathway activation is associated with cetuximab resistance and EPHB3 receptor induction in colorectal cancer. Theranostics. 2019 Apr 12;9(8):2235-2251. [Content Brief]
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). 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 | 2.2478 mL | 11.2392 mL | 22.4785 mL | 56.1962 mL |
| 5 mM | 0.4496 mL | 2.2478 mL | 4.4957 mL | 11.2392 mL | |
| 10 mM | 0.2248 mL | 1.1239 mL | 2.2478 mL | 5.6196 mL | |
| 15 mM | 0.1499 mL | 0.7493 mL | 1.4986 mL | 3.7464 mL | |
| 20 mM | 0.1124 mL | 0.5620 mL | 1.1239 mL | 2.8098 mL | |
| 25 mM | 0.0899 mL | 0.4496 mL | 0.8991 mL | 2.2478 mL | |
| 30 mM | 0.0749 mL | 0.3746 mL | 0.7493 mL | 1.8732 mL | |
| 40 mM | 0.0562 mL | 0.2810 mL | 0.5620 mL | 1.4049 mL | |
| 50 mM | 0.0450 mL | 0.2248 mL | 0.4496 mL | 1.1239 mL | |
| 60 mM | 0.0375 mL | 0.1873 mL | 0.3746 mL | 0.9366 mL | |
| 80 mM | 0.0281 mL | 0.1405 mL | 0.2810 mL | 0.7025 mL | |
| 100 mM | 0.0225 mL | 0.1124 mL | 0.2248 mL | 0.5620 mL |
LDN-211904 oxalate Related Classifications
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