PPI-GIT1/β-Pix PPI-IN-1
Based on 1 Customer Validation
PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a KD value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer.
For research use only. We do not sell to patients.
- Purity: 99.01%
- CAS No.: 2070916-70-8
- Formula: C23H21NO5
- Molecular Weight:391.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 0-50 μM) inhibits the interaction between GIT1 and β-Pix in living cells[1].
PPI-GIT1/β-Pix interaction-IN-1 (0-50 μM; 24 h; MGC803 cells and MKN45 cells) inhibits gastric cancer cell invasion in a dose-dependent manner and disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MGC803 cells and MKN45 cells
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Concentration:0, 5, 20, and 50 μM
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Incubation Time:24 hours
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Result:Suppressed the expression of GTP-Rac1 and GTP-Cdc42 in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice with MGC803 xenografts (Four-week-old)[1]
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Dosage:10 and 30 mg/kg
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Administration:oral gavage, daily, for 18 days
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Result:Reduced the luminescence intensity in the lungs in a dose-dependent manner.
Chemical Information
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CAS No. 2070916-70-8
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Appearance Solid
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Molecular Weight 391.42
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Formula C23H21NO5
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Color White to light brown
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SMILES
O=C([C@@H]1[C@@H](C(OCC)=O)[C@]2(C(N(C)C3=C2C=CC=C3)=O)[C@H]/4C1)C4=C\C5=COC=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (255.48 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. 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: ≥ 2.5 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 2.5548 mL | 12.7740 mL | 25.5480 mL | 63.8700 mL |
| 5 mM | 0.5110 mL | 2.5548 mL | 5.1096 mL | 12.7740 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5548 mL | 6.3870 mL | |
| 15 mM | 0.1703 mL | 0.8516 mL | 1.7032 mL | 4.2580 mL | |
| 20 mM | 0.1277 mL | 0.6387 mL | 1.2774 mL | 3.1935 mL | |
| 25 mM | 0.1022 mL | 0.5110 mL | 1.0219 mL | 2.5548 mL | |
| 30 mM | 0.0852 mL | 0.4258 mL | 0.8516 mL | 2.1290 mL | |
| 40 mM | 0.0639 mL | 0.3194 mL | 0.6387 mL | 1.5968 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5110 mL | 1.2774 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4258 mL | 1.0645 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3194 mL | 0.7984 mL | |
| 100 mM | 0.0255 mL | 0.1277 mL | 0.2555 mL | 0.6387 mL |
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