LDN-211904 |
| Catalog No.GC16798 |
LDN-211904 (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 μM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1198408-78-4
Sample solution is provided at 25 µL, 10mM.
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IC50: 79 nM for EphB3
LDN-211904 is an inhibitor of erythropoietin-producing hepatocellular carcinoma (Eph) receptors.
Erythropoietin-producing hepatocellular carcinoma (Eph) receptors, a group of highly conserved transmembrane proteins composed of multiple domains, participate in various cell signaling pathways. So far, 16 Eph receptors have been identified in vertebrates, which can be divided into two major classes (EphA and EphB) based on sequence similarity. Mammals including humans have 14 Eph receptors (EphA1–EphA8, EphA10, EphB1–EphB4 and EphB6).
In vitro: Previous study found that LDN-211904, a 4-piperidinyl analog, retained significant EphB3 inhibitory activity, and also had greater aqueous solubility due to the presence of a basic amine. LDN-211904 was profiled for functional inhibitory activity against a panel of 288 kinases and the results showed that LDN-211904 was quite selective for tyrosine kinases. The only noted exceptions were the three serine/threonine kinases p38a, p38b, and Qik. In addition, only LDN-211904 showed moderate selectivity among the tyrosine kinases and little selectivity verses other EphA and EphB subtypes, except for EphA6 and EphA7. Moreover, LDN-211904 demonstrated the best stability with a t1/2 of 348 min and a CLint of 4 μL/min/mg protein [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Qiao, L. ,Choi, S.,Case, A., et al. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Bioor. Med. Chem. Lett. 19(21), 6122-6126 (2009).
| Cas No. | 1198408-78-4 | SDF | |
| Chemical Name | N-(2-chlorophenyl)-6-(4-piperidinyl)-imidazo[1,2-a]pyridine-3-carboxamide, monoethanedioate | ||
| Canonical SMILES | O=C(NC1=C(Cl)C=CC=C1)C2=CN=C(C=C3)N2C=C3C4CCNCC4.OC(C(O)=O)=O | ||
| Formula | C19H19ClN4O • C2H2O4 | M.Wt | 444.9 |
| Solubility | ≤20mg/ml in DMSO;0.5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2477 mL | 11.2385 mL | 22.477 mL |
| 5 mM | 0.4495 mL | 2.2477 mL | 4.4954 mL |
| 10 mM | 0.2248 mL | 1.1238 mL | 2.2477 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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