SPI-112
Based on 1 publication(s) in Google Scholar
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.
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: 98.01%
- CAS 番号: 1051387-90-6
- 分子式: C22H17FN4O5S
- 分子量:468.46
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
MedChemExpress(MCE)の使用を引用している文献 SPI-112
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生物活性
製品説明
IC50 & Target
IC50: 1 μM (SHP2), 18.3 μM (PTP) and 14.5 μM (PTP1B)[2]
体外実験
SPI-112 has a polar -NO2 or a negatively charged -COOH group and has no detectable cellular activity, suggesting that SPI-112 is not cell permeable[1].
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In surface plasmon resonance (SPR) binding assay, SPI-112 displays a 1:1 stoichiometric binding kinetics to SHP2 with a kinetic constant KD of 1.30 μM. Enzyme kinetic data obtained with SPI-112 are best fitted with the competitive inhibition model (Ki of 0.8 μM), suggesting that SPI-112 interacts with the catalytic site of SHP2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1051387-90-6
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性状 Solid
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分子量 468.46
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分子式 C22H17FN4O5S
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Color Light yellow to brown
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SMILES
O=C(O)C1=CC=CC(N/N=C2C(NC3=C\2C=C(S(=O)(NCC4=CC=C(F)C=C4)=O)C=C3)=O)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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EMBO Mol Med
Modulating CCTG repeat expansion toxicity in DM2 Drosophila model through TDP1 inhibition. [Abstract]2025 Mar 25. PMID: 40133672
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (106.73 mM; Need ultrasonic; 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 (protect from light). 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 (protect from light). 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 (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chen L, et al. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112. Biochem Pharmacol. 2010 Sep 15;80(6):801-10. [Content Brief]
[2]. Lawrence HR, et al. Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. J Med Chem. 2008 Aug 28;51(16):4948-56. [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 (protect from light). 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 | 2.1347 mL | 10.6733 mL | 21.3465 mL | 53.3664 mL |
| 5 mM | 0.4269 mL | 2.1347 mL | 4.2693 mL | 10.6733 mL | |
| 10 mM | 0.2135 mL | 1.0673 mL | 2.1347 mL | 5.3366 mL | |
| 15 mM | 0.1423 mL | 0.7116 mL | 1.4231 mL | 3.5578 mL | |
| 20 mM | 0.1067 mL | 0.5337 mL | 1.0673 mL | 2.6683 mL | |
| 25 mM | 0.0854 mL | 0.4269 mL | 0.8539 mL | 2.1347 mL | |
| 30 mM | 0.0712 mL | 0.3558 mL | 0.7116 mL | 1.7789 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5337 mL | 1.3342 mL | |
| 50 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL | |
| 60 mM | 0.0356 mL | 0.1779 mL | 0.3558 mL | 0.8894 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6671 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2135 mL | 0.5337 mL |