UniPR129
Based on 1 Customer Validation
UniPR129 is a potent and orally active Eph/ephrin antagonist. UniPR129 can inhibit EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. UniPR129 can inhibit angiogenesis and show antitumor and neuroprotective effect. UniPR129 can be used for the researches of cancer and neurological disease, such as colorectal cancer and optic neuropathy.
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- Purity: 99.23%
- CAS No.: 1639159-47-9
- 화학식: C36H52N2O4
- 분자량:576.81
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보관:Powder -20°C, 3 years , 4°C, 2 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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Kinase Inhibitor Library
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Neuroprotective Compound Library
HY-L070
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Angiogenesis-Related Compound Library
HY-L088
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Anti-Colorectal Cancer Compound Library
HY-L103
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
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Cell Proliferation Compound Library
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High-Throughput Bioactive Compound Library
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Posttranslational Modification Library
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Biological Activity
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EphA8 0.84 μM (IC50) |
EphA2 1.12 μM (IC50) |
EphA7 1.24 μM (IC50) |
EphA1 1.39 μM (IC50) |
EphA3 1.43 μM (IC50) |
EphA6 1.53 μM (IC50) |
EphA5 1.57 μM (IC50) |
EphA4 1.58 μM (IC50) |
EphB4 2.60 μM (IC50) |
EphB1 2.75 μM (IC50) |
EphB2 2.96 μM (IC50) |
EphB5 3.01 μM (IC50) |
EphB3 3.74 μM (IC50) |
UniPR129 (1.5-25 μM, 20 mins) inhibits EphA2 activation in PC3 cells[1].
UniPR129 (6-50 μM, 2 h) does not show any toxic effect in PC3 cells[1].
UniPR129 (1.56-12.5, 20 mins) inhibits PC3 cells retraction[1].
UniPR129 (1.5-25, 15 h) inhibits angiogenesis in HUVECs[1].
UniPR129 (50 μM) shows neuroprotection in retinas isolated from optic nerve crush (ONC) injury mices model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:1.56, 3.12, 6.25 and 12.5 μM
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Incubation Time:20 mins
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Result:Inhibited the rounding effect of ephrin-A1-Fc
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APC min/J mice[2]
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Dosage:30 mg/kg
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Administration:Orally administration, every other day for 8 weeks
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Result:Reduced the formation of adenomas in the ileum of 1.6 times.
Reduced tumor volume.
Chemical Information
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CAS No. 1639159-47-9
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Appearance Solid
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분자량 576.81
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화학식 C36H52N2O4
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Color White to off-white
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SMILES
C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(N[C@H](CC(O)=O)CC3=CNC4=CC=CC=C34)=O)([H])[C@@]5([H])[C@]([C@@]6([C@](C[C@H](O)CC6)([H])CC5)C)([H])CC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 33.33 mg/mL (57.78 mM; ultrasonic and warming and heat to 60°C; 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)
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Hassan-Mohamed I, et al. UniPR129 is a competitive small molecule Eph-ephrin antagonist blocking in vitro angiogenesis at low micromolar concentrations. Br J Pharmacol. 2014 Dec;171(23):5195-208. [Content Brief]
[2]. Corrado M, et al. Evaluation of the Anti-Tumor Activity of Small Molecules Targeting Eph/Ephrins in APC min/J Mice. Pharmaceuticals (Basel). 2020 Apr 16;13(4):69. [Content Brief]
[3]. Strong TA, et al. Activation of multiple Eph receptors on neuronal membranes correlates with the onset of optic neuropathy. Eye Vis (Lond). 2023 Oct 2;10(1):42. [Content Brief]
[4]. Giorgio C, et al. Pharmacological evaluation of new bioavailable small molecules targeting Eph/ephrin interaction. Biochem Pharmacol. 2018 Jan;147:21-29. [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. 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 | 1.7337 mL | 8.6684 mL | 17.3367 mL | 43.3418 mL |
| 5 mM | 0.3467 mL | 1.7337 mL | 3.4673 mL | 8.6684 mL | |
| 10 mM | 0.1734 mL | 0.8668 mL | 1.7337 mL | 4.3342 mL | |
| 15 mM | 0.1156 mL | 0.5779 mL | 1.1558 mL | 2.8895 mL | |
| 20 mM | 0.0867 mL | 0.4334 mL | 0.8668 mL | 2.1671 mL | |
| 25 mM | 0.0693 mL | 0.3467 mL | 0.6935 mL | 1.7337 mL | |
| 30 mM | 0.0578 mL | 0.2889 mL | 0.5779 mL | 1.4447 mL | |
| 40 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0835 mL | |
| 50 mM | 0.0347 mL | 0.1734 mL | 0.3467 mL | 0.8668 mL |
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