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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.23%
- CAS 番号: 1639159-47-9
- 分子式: C36H52N2O4
- 分子量:576.81
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Kinase Inhibitor Library
HY-L009
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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
HY-L149
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Membrane Receptor-targeted Compound Library
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Multi-Target Compound Library
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Bioactive Compound Library Max
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Bioactive Compound Library
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Protein Kinase 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
HY-L226
生物活性
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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.
化学情報
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CAS 番号 1639159-47-9
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性状 Solid
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分子量 576.81
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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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