PPI-2458
Based on 1 Customer Validation
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma 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: 99.67%
- CAS 番号: 431077-35-9
- 分子式: C22H36N2O6
- 分子量:424.53
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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生物活性
PPI-2458 potently inhibits HUVEC proliferation with a GI50 of 0.2 nM and a maximum inhibition of >95% at 1 nM[1].
PPI-2458 (0-100 nM, 6 days) inhibits proliferation and MetAP-2 in SU-DHL-16 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DHL-16 cells
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Concentration:0, 0.01, 0.1, 1, 10, and 100 nM
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Incubation Time:6 days
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Result:Inhibited SU-DHL-16 proliferation in a dose-dependent fashion with maximum inhibition of 60% achieved at the highest concentration (100 nmol/L) and GI50 at 1.9 nmol/L.
PPI-2458 (0-3 mg/kg, Nasogastric intubation, qod) shows a decrease in germinal center lymphocytes in experimentally naive cynomolgus monkeys[2].
PPI-2458 (0-100 mg/kg, Orally, qod) significantly suppresses tumor growth in a dose-dependent manner in severe combined immunodeficient mice with SR tumor xenografts [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)[1]
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Dosage:0.25, 1, 5, and 50 mg/kg
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Administration:Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
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Result:Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.
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Animal Model:Forty-two experimentally naive cynomolgus monkeys[2]
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Dosage:0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
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Administration:Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
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Result:Exhibited a marked decrease in germinal center lymphocytes.
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Animal Model:60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)[2]
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Dosage:10, 30, or 100 mg/kg
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Administration:oral gavage, QOD
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Result:Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 431077-35-9
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性状 Solid
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分子量 424.53
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分子式 C22H36N2O6
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Color White to off-white
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SMILES
O=C(O[C@H](CC1)[C@@H](OC)[C@H]([C@@]2(C)O[C@@H]2C/C=C(C)\C)[C@]31CO3)N[C@@H](C(N)=O)C(C)C
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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 : ≥ 100 mg/mL (235.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
純度とドキュメンテーション
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データシート (276 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bernier SG, et al. A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis. Proc Natl Acad Sci U S A. 2004 Jul 20;101(29):10768-73. [Content Brief]
[2]. Cooper AC, et al. A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo. Clin Cancer Res. 2006 Apr 15;12(8):2583-90. [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 | 2.3555 mL | 11.7777 mL | 23.5555 mL | 58.8887 mL |
| 5 mM | 0.4711 mL | 2.3555 mL | 4.7111 mL | 11.7777 mL | |
| 10 mM | 0.2356 mL | 1.1778 mL | 2.3555 mL | 5.8889 mL | |
| 15 mM | 0.1570 mL | 0.7852 mL | 1.5704 mL | 3.9259 mL | |
| 20 mM | 0.1178 mL | 0.5889 mL | 1.1778 mL | 2.9444 mL | |
| 25 mM | 0.0942 mL | 0.4711 mL | 0.9422 mL | 2.3555 mL | |
| 30 mM | 0.0785 mL | 0.3926 mL | 0.7852 mL | 1.9630 mL | |
| 40 mM | 0.0589 mL | 0.2944 mL | 0.5889 mL | 1.4722 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1778 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9815 mL | |
| 80 mM | 0.0294 mL | 0.1472 mL | 0.2944 mL | 0.7361 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL |
PPI-2458 関連分類
HY-13731 関連分類
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