DCAI
Based on 1 Customer Validation
DCAI is a KRas inhibitor with a Kd value of 1.1 mM. DCAI directly binds to the Ras protein and competitively inhibits SOS-mediated nucleotide release (IC50 = 155 μM) and exchange reaction (IC50 = 342 μM). DCAI binds to the pocket at the Ras-SOS interface and blocks the formation of the Ras-SOS complex intermediate by impeding salt bridge formation through steric hindrance and the induction of Ras conformational changes. DCAI is used in the study of wild-type and mutant Ras tumors.
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- No. CAS: 299165-92-7
- Fòrmula: C11H12Cl2N2
- Peso molecular:243.13
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[2]|
K-RAS 1.1 mM (Kd) |
In Vitro
DCAI (pre-incubation for 5 min; detection duration of 30 min) hydrochloride potently inhibits SOScat-catalyzed guanine nucleotide exchange of purified KRasGDP protein, with a mean IC50 of 342 μM.
DCAI (25 μM) hydrochloride does not affect the localization of full-length Ras at the cell membrane, nor does it cause widespread disruption of plasma membrane protein interactions in HEK-293T cells[2].
DCAI hydrochloride (100 μM; 2 h) reduces EGF (HY-P7109)-stimulated endogenous RasGTP levels in HEK 293T cells[2].
DCAI hydrochloride blocks the plasma membrane aggregation of fluorescent probes containing the cRaf RBD-CRD domain in HEK-293T cells (EC50 = 15.8 μM) and inhibits endogenous Ras activation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:HEK-293T
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Concentration:100 μM
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Incubation Time:treatment for 2 hours followed by EGF stimulation for 5 minutes
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Result:Attenuated the Ras activation induced by EGF stimulation.
Chemical Information
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No. CAS 299165-92-7
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Appearance Solid
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Peso molecular 243.13
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Fòrmula C11H12Cl2N2
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Color Light yellow to yellow
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SMILES
CC(NC1=C2C(Cl)=CC(Cl)=C1)=C2CCN
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (411.30 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)
In Vivo:
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 (10.28 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.28 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 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 4.1130 mL | 20.5651 mL | 41.1303 mL | 102.8256 mL |
| 5 mM | 0.8226 mL | 4.1130 mL | 8.2261 mL | 20.5651 mL | |
| 10 mM | 0.4113 mL | 2.0565 mL | 4.1130 mL | 10.2826 mL | |
| 15 mM | 0.2742 mL | 1.3710 mL | 2.7420 mL | 6.8550 mL | |
| 20 mM | 0.2057 mL | 1.0283 mL | 2.0565 mL | 5.1413 mL | |
| 25 mM | 0.1645 mL | 0.8226 mL | 1.6452 mL | 4.1130 mL | |
| 30 mM | 0.1371 mL | 0.6855 mL | 1.3710 mL | 3.4275 mL | |
| 40 mM | 0.1028 mL | 0.5141 mL | 1.0283 mL | 2.5706 mL | |
| 50 mM | 0.0823 mL | 0.4113 mL | 0.8226 mL | 2.0565 mL | |
| 60 mM | 0.0686 mL | 0.3428 mL | 0.6855 mL | 1.7138 mL | |
| 80 mM | 0.0514 mL | 0.2571 mL | 0.5141 mL | 1.2853 mL | |
| 100 mM | 0.0411 mL | 0.2057 mL | 0.4113 mL | 1.0283 mL |
DCAI Related Classifications
HY-118692 Related Classifications
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