PRT-060318
Based on 4 publication(s) in Google Scholar
PRT-060318 (PRT318) s a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 prevents Heparin (HY-17567)-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.
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: 99.59%
- CAS 番号: 1194961-19-7
- 分子式: C18H24N6O
- 分子量:340.42
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 PRT-060318
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生物活性
PRT-060318 (PRT318) (0-3 µM, 15 min) completely inhibits Heparin-induced thrombocytopenia (HIT) immune complex-induced aggregation of both human and transgenic HIT mouse platelets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 mice treated with KKO (20 mg/kg, i.p.)[1]
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Dosage:10 and 30 mg/kg
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Administration:i.g., b.i.d. for 7 days
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Result:Significantly inhibited platelet deposition without affecting bleeding time.
Markedly reduced HIT immune complex-induced thrombosis in the lungs.
Significantly reduced the thrombosis score compared to vehicle.
化学情報
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CAS 番号 1194961-19-7
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性状 Solid
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分子量 340.42
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分子式 C18H24N6O
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Color Light yellow to yellow
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SMILES
O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N
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別名
PRT318
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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 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Environ Pollut
Investigating the role and mechanism of methionine in different types of skeletal fluorosis based on Siglec-15 methylation. [Abstract]2026 Feb 1:390:127432. PMID: 41349947 -
FASEB J
Receptor-Dependent and -Independent Effects of Hemin on Platelet Plasma Membrane Disintegration. [Abstract]2026 Jan 31;40(2):e71463. PMID: 41524235 -
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溶剤 & 溶解度
H2O : 25 mg/mL (73.44 mM; Need ultrasonic)
DMSO : 10 mg/mL (29.38 mM; ultrasonic and warming and adjust pH to 3 with 1 M HCl 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (73.44 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (277 KB)
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SDS (406 KB)
- English - EN (406 KB)
- Français - FR (406 KB)
- Deutsch - DE (406 KB)
- Norwegian - NO (406 KB)
- Español - ES (406 KB)
- Swedish - SV (406 KB)
- Italian - IT (406 KB)
- Korean - KR (406 KB)
- Portuguese - PT (406 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Reilly MP, et al. PRT-060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. Blood. 2011 Feb 17;117(7):2241-6. [Content Brief]
[2]. Hoellenriegel J, et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL | 73.4387 mL |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 14.6877 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL | 7.3439 mL | |
| 15 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8959 mL | |
| 20 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6719 mL | |
| 25 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9375 mL | |
| H2O | 30 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL |
| 40 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8360 mL | |
| 50 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.