| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
LDN-211904 oxalate selectively targets EphB3 (Erythropoietin-producing hepatocellular carcinoma B3), a receptor tyrosine kinase involved in cell migration, adhesion, and tumor progression. The compound shows good selectivity for EphB3 based on profiling against a panel of 288 kinases.
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|---|---|
| ln Vitro |
LDN-211904 oxalate potently inhibits EphB3 with an IC50 of 0.079 microM. It shows good metabolic stability in mouse liver microsomes. The combination of LDN-211904 oxalate with cetuximab is effective in inhibiting STAT3-activated cancer stem cell stemness and overcoming cetuximab resistance in colorectal cancer.
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| ln Vivo |
In vivo, LDN-211904 oxalate is administered at 0.1 mg/kg by intraperitoneal injection three times weekly for 21 days. This regimen inhibits and overcomes acquired cetuximab resistance in tumor xenograft models, demonstrating antitumor efficacy when combined with cetuximab.
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| Enzyme Assay |
The inhibitory activity against EphB3 is measured using an in vitro kinase assay with recombinant EphB3 enzyme and a peptide substrate. The phosphorylation level is quantified using a luminescence-based method. The IC50 is calculated by plotting inhibition percentage against varying compound concentrations.
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| Cell Assay |
Colorectal cancer cell lines (e.g., cetuximab-resistant cells) are cultured and treated with varying concentrations of LDN-211904 oxalate. Cell viability is measured by MTT or CellTiter-Glo assays. Cancer stem cell markers and STAT3 activation are assessed by Western blot.
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| Animal Protocol |
A tumor xenograft model is established in immunodeficient mice. Cetuximab-resistant tumor cells are implanted subcutaneously. Once tumors reach a certain size, mice are administered LDN-211904 oxalate via intraperitoneal injection (0.1 mg/kg, three times weekly for 21 days). Tumor volumes are measured regularly.
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| ADME/Pharmacokinetics |
LDN-211904 oxalate demonstrates good metabolic stability in mouse liver microsomes, suggesting favorable hepatic clearance characteristics. Detailed PK parameters such as half-life, oral bioavailability, and plasma protein binding are not extensively reported in standard profiles.
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| Toxicity/Toxicokinetics |
Detailed toxicological studies for LDN-211904 oxalate are not extensively documented in standard profiles. As a research-grade compound, comprehensive acute and sub-chronic toxicity evaluations have not been publicly reported. Standard laboratory safety precautions apply.
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| References |
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| Additional Infomation |
LDN-211904 oxalate is identified as compound 32 in the original research. It is strictly for research use and is not an approved drug. Its ability to target EphB3 makes it a valuable tool for studying tyrosine kinase signaling, cancer stem cell biology, and acquired resistance mechanisms.
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| Molecular Formula |
C21H21CLN4O5
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|---|---|
| Molecular Weight |
444.868243932724
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| Exact Mass |
444.12
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| CAS # |
1198408-78-4
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| Related CAS # |
LDN-211904; 1198408-39-7; LDN-211904 oxalate; 1198408-78-4
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| PubChem CID |
46882744
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| Appearance |
White to off-white solid powder
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| LogP |
3.264
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
542
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CNCCC1C2=CN3C(=NC=C3C(=O)NC4=CC=CC=C4Cl)C=C2.C(=O)(C(=O)O)O
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| InChi Key |
ODBJGLKPAQMCJA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19ClN4O.C2H2O4/c20-15-3-1-2-4-16(15)23-19(25)17-11-22-18-6-5-14(12-24(17)18)13-7-9-21-10-8-13;3-1(4)2(5)6/h1-6,11-13,21H,7-10H2,(H,23,25);(H,3,4)(H,5,6)
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| Chemical Name |
N-(2-chlorophenyl)-6-piperidin-4-ylimidazo[1,2-a]pyridine-3-carboxamide;oxalic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~224.8 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2478 mL | 11.2392 mL | 22.4785 mL | |
| 5 mM | 0.4496 mL | 2.2478 mL | 4.4957 mL | |
| 10 mM | 0.2248 mL | 1.1239 mL | 2.2478 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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