Pan-RAS-IN-2
Based on 1 Customer Validation
Pan-rasin-2 (compound 6A) is an orally active molecular glues that targets RAS. Pan-RAS-IN-2 inhibits pERK (IC50 in AsPC-1 cells: 0.3 nM). Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor (such as colorectal cancer, pancreatic cancer) effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.74%
- CAS. Nr.: 3034673-92-9
- Formel: C46H60N8O5S
- Molecular Weight:837.08
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Alle Cyclophilin Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
IC50 in AsPC-1 cells: 0.3 nM (pERK)[1]
Pan-RAS-IN-2 significantly inhibits the proliferation of RAS mutant cells GP2D, PK-59, AsPC-1, PSN-1, RKN, Capan-1, SW620, and HCT116, with IC50 values of 0.9 nM, 2.3 nM, 2.1 nM, 5.3 nM, 4.5 nM, 2.5 nM, 0.2 nM, and 5.5 nM, respectively[1].
Pan-RAS-IN-2 also inhibits pERK in AsPC-1 cells, with an IC50 of 0.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pan-RAS-IN-2 (0.5-5 mg/kg; p.o.) demonstrates excellent antitumor effects in nude mice with pancreatic cancer[1].
Pan-RAS-IN-2 (1-10 mg/kg; in rats: i.v. (1 mg/kg) or p.o. (10 mg/kg); in beagles: i.v. (1 mg/kg) or p.o. (5 mg/kg)) has a long half-life in male SD rats and beagles, with T1/2 values of 5.7 h (rat, intravenous injection), 6.1 h (rat, gavage), 24.5 h (beagles, intravenous injection), and 22.4 h (beagles, gavage), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3034673-92-9
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Appearance Solid
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Molecular Weight 837.08
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Formel C46H60N8O5S
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Color White to light yellow
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SMILES
O=C1OCC(C)(CC2=[C@@]([C@@]3=C([C@H](C)OC)N=CC(N4CCN(C)CC4)=C3)N(CC)C5=CC=C(C6=CSC(C[C@H](NC([C@H]7[C@H](C)[C@@H]7C)=O)C(N8N[C@H]1C9CC8C9)=O)=N6)C=C25)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (119.46 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (2.99 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.
Reinheit & Dokumentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
Verweise
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 | 1.1946 mL | 5.9731 mL | 11.9463 mL | 29.8657 mL |
| 5 mM | 0.2389 mL | 1.1946 mL | 2.3893 mL | 5.9731 mL | |
| 10 mM | 0.1195 mL | 0.5973 mL | 1.1946 mL | 2.9866 mL | |
| 15 mM | 0.0796 mL | 0.3982 mL | 0.7964 mL | 1.9910 mL | |
| 20 mM | 0.0597 mL | 0.2987 mL | 0.5973 mL | 1.4933 mL | |
| 25 mM | 0.0478 mL | 0.2389 mL | 0.4779 mL | 1.1946 mL | |
| 30 mM | 0.0398 mL | 0.1991 mL | 0.3982 mL | 0.9955 mL | |
| 40 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7466 mL | |
| 50 mM | 0.0239 mL | 0.1195 mL | 0.2389 mL | 0.5973 mL | |
| 60 mM | 0.0199 mL | 0.0996 mL | 0.1991 mL | 0.4978 mL | |
| 80 mM | 0.0149 mL | 0.0747 mL | 0.1493 mL | 0.3733 mL | |
| 100 mM | 0.0119 mL | 0.0597 mL | 0.1195 mL | 0.2987 mL |
Pan-RAS-IN-2 Related Classifications
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