Erasin
Based on 2 publication(s) in Google Scholar
Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis.
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- Pureté: 96.02%
- CAS No.: 2256056-21-8
- Formule: C20H19N3O3
- Masse moléculaire:349.38
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Stockage: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
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Erasin
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Activité biologique
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STAT3 9.7 μM (IC50) |
STAT1 24 μM (IC50) |
Erasin inhibits protein-protein interactions mediated by STAT SH2 domains[1].
Erasin (0-80 μM; 24 h) induces apoptosis in MDA-MB-231, HCC-827 and Erlotinib (HY-50896)-resistant HCC-827 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and K562 cells
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Concentration:0, 5, 10, 25, 50 and 100 μM
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Incubation Time:24 h (pretreated for 1-2h)
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Result:Inhibited interleukin (IL)-6-stimulated STAT3 Tyr705 phosphorylation in HepG2 cells in a dose-dependent manner. Interferon (IFN)-γ-stimulated phosphorylation of STAT1 Tyr701 was inhibited to a lesser extent. Tyrosine phosphorylation of STAT5 in K562 cells was not inhibited.
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Cell Line:MDA-MB-231, HCC-827, Erlotinib (HY-50896)-resistant HCC-827 and MDA-MB-453 cells
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Concentration:0, 20, 40, 60 and 80 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in the rate of apoptosis in MDA-MB-231 and HCC-827 cells, compared to DMSO-treated control cells. Was equally effective at increasing the apoptotic rate of Erlotinib-resistant HCC-827 cells and parental HCC-827 cells compared to the respective DMSO-treated control cells.
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Cell Line:Parental HCC-827 cells and Erlotinib (HY-50896)-resistant HCC-827 cells
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Concentration:0, 20, 40, 60 and 80 μM
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Incubation Time:24 h (pretreated for 1-2h)
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Result:Showed a dose-dependent inhibitory effect on STAT3 Tyr705 phosphorylation in both parental HCC-827 and Erlotinib-resistant HCC-827 cells.
Chemical Information
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CAS No. 2256056-21-8
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Appearance Solid
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Masse moléculaire 349.38
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Formule C20H19N3O3
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Color Off-white to light yellow
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SMILES
O=C(N/N=C/C1=COC(C=CC(C(C)(C)C)=C2)=C2C1=O)C3=CC=CN=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
Solvant et solubilité
DMSO : 62.5 mg/mL (178.89 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
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 | 2.8622 mL | 14.3111 mL | 28.6221 mL | 71.5553 mL |
| 5 mM | 0.5724 mL | 2.8622 mL | 5.7244 mL | 14.3111 mL | |
| 10 mM | 0.2862 mL | 1.4311 mL | 2.8622 mL | 7.1555 mL | |
| 15 mM | 0.1908 mL | 0.9541 mL | 1.9081 mL | 4.7704 mL | |
| 20 mM | 0.1431 mL | 0.7156 mL | 1.4311 mL | 3.5778 mL | |
| 25 mM | 0.1145 mL | 0.5724 mL | 1.1449 mL | 2.8622 mL | |
| 30 mM | 0.0954 mL | 0.4770 mL | 0.9541 mL | 2.3852 mL | |
| 40 mM | 0.0716 mL | 0.3578 mL | 0.7156 mL | 1.7889 mL | |
| 50 mM | 0.0572 mL | 0.2862 mL | 0.5724 mL | 1.4311 mL | |
| 60 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1926 mL | |
| 80 mM | 0.0358 mL | 0.1789 mL | 0.3578 mL | 0.8944 mL | |
| 100 mM | 0.0286 mL | 0.1431 mL | 0.2862 mL | 0.7156 mL |
Erasin Related Classifications
HY-115594 Related Classifications
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