| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Eph inhibitor 2 targets members of the Eph family of receptor tyrosine kinases. Eph receptors and their ephrin ligands are involved in a wide range of biological processes, including cell migration, adhesion, and angiogenesis. By inhibiting Eph receptor kinase activity, this compound blocks downstream signaling pathways that can contribute to tumor progression and other pathological conditions.
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|---|---|
| ln Vitro |
In vitro, Eph inhibitor 2 has been shown to inhibit Eph family tyrosine kinase activity. While specific IC50 values are not widely published, its activity is typically assessed using kinase assays that measure the phosphorylation of a substrate in the presence of the compound. These studies confirm its potential as a tool for studying Eph receptor signaling.
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| ln Vivo |
In vivo activity of Eph inhibitor 2 is not extensively documented. As a research compound, its efficacy is typically evaluated in animal models of diseases where Eph receptor signaling plays a role, such as cancer. By inhibiting Eph receptors, it may suppress tumor growth, angiogenesis, and metastasis. Further studies are needed to fully characterize its in vivo effects.
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| Enzyme Assay |
Cell-free assays for Eph inhibitor 2 typically involve measuring its inhibitory activity against Eph family kinases using biochemical kinase assays. The compound's IC50 value is determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the inhibitor. These assays are used to characterize the compound's potency and selectivity against Eph receptors.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Eph inhibitor 2. Cancer cell lines or other cell types expressing Eph receptors are treated with the compound. Cell proliferation, migration, and invasion are measured to assess the compound's effects on Eph-mediated cellular processes. Eph receptor phosphorylation is also measured to confirm inhibition of the target kinases.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of cancer or other disease models where Eph receptors play a role. Animals are administered Eph inhibitor 2. Tumor growth, angiogenesis, or other disease parameters are monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo activity of the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Eph inhibitor 2 are typical of a small molecule inhibitor. Its molecular weight is 317.34. It is soluble in DMSO at 32.5 mg/mL. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics, including good permeability and metabolic stability.
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| Toxicity/Toxicokinetics |
The toxicity profile of Eph inhibitor 2 is not extensively documented but is likely to be similar to other kinase inhibitors. Common adverse effects may include fatigue, diarrhea, and nausea. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins and identify potential target organ toxicities.
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| References | |
| Additional Infomation |
Eph inhibitor 2 is a research compound targeting Eph family tyrosine kinases. It is used to study Eph receptor signaling pathways and their role in various diseases, including cancer. The compound is not approved for therapeutic use and is intended for research purposes only.
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| Molecular Formula |
C18H15N5O
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|---|---|
| Molecular Weight |
317.34
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| Exact Mass |
317.127
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| CAS # |
861249-59-4
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| PubChem CID |
11594862
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| Appearance |
White to off-white solid
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
422
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC(=C1)C2=C(N3C(=C(C=N3)C4=CN=CC=C4)N=C2)N
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| InChi Key |
KWGYGRTZRXWSAD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15N5O/c1-24-14-6-2-4-12(8-14)15-10-21-18-16(11-22-23(18)17(15)19)13-5-3-7-20-9-13/h2-11H,19H2,1H3
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| Chemical Name |
6-(3-methoxyphenyl)-3-pyridin-3-ylpyrazolo[1,5-a]pyrimidin-7-amine
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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 |
| 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: ~25 mg/mL (~78.8 mM; with ultrasonication and warming by heating to 60°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.88 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 (7.88 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1512 mL | 15.7560 mL | 31.5119 mL | |
| 5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL | |
| 10 mM | 0.3151 mL | 1.5756 mL | 3.1512 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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