SHP394
Based on 1 publication(s) in Google Scholar
SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM.
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- 純度: 99.66%
- CAS 番号: 2055757-40-7
- 分子式: C20H25F3N6O2S
- 分子量:470.51
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 SHP394
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生物活性
IC50: 23 nM (SHP2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Detroit 562 | IC50 |
1.38 μM
Compound: 1; SHP394
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Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay
Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay
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[PMID: 30688459] |
| KYSE-520 cell line | IC50 |
0.297 μM
Compound: 1; SHP394
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Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay
Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay
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[PMID: 30688459] |
SHP394 inhibits Caco-2 cells proliferation with the IC50 of 297 nM[1].
SHP394 exhibits antiproliferation activity against the Detroit-562 pharyngeal carcinoma cell line in vitro (IC50= 1.38 μM) [1].
SHP394 decreases p-ERK with an IC50 of 18 nM KYSE520 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SHP394 (80 mg/kg; oral gavage; twice daily) causes tumor 34% regression and reduces mouse host bodyweight after dosing for 14 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week old female athymic NU/NU mice were inoculated subcutaneously with Detroit-562 pharyngeal carcinoma cells[1].
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Dosage:20, 40, and 80 mg/kg
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Administration:Oral gavage; twice daily
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Result:Demonstrated a clear dose-dependent reduction in tumor volume.
化学情報
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CAS 番号 2055757-40-7
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性状 Solid
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分子量 470.51
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分子式 C20H25F3N6O2S
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Color White to off-white
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SMILES
NC1=C(C(N(C)C(N2CCC3(CO[C@@H](C)[C@H]3N)CC2)=N1)=O)SC4=C(C(F)(F)F)N=CC=C4
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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, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 24 mg/mL (51.01 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (13.28 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6.25 mg/mL (13.28 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
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- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 (stored under nitrogen). 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 | 2.1254 mL | 10.6268 mL | 21.2535 mL | 53.1338 mL |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2507 mL | 10.6268 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 mL | 5.3134 mL | |
| 15 mM | 0.1417 mL | 0.7085 mL | 1.4169 mL | 3.5423 mL | |
| 20 mM | 0.1063 mL | 0.5313 mL | 1.0627 mL | 2.6567 mL | |
| 25 mM | 0.0850 mL | 0.4251 mL | 0.8501 mL | 2.1254 mL | |
| 30 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.7711 mL | |
| 40 mM | 0.0531 mL | 0.2657 mL | 0.5313 mL | 1.3283 mL | |
| 50 mM | 0.0425 mL | 0.2125 mL | 0.4251 mL | 1.0627 mL |