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SOS1-IN-21
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Catalog No. T212275Cas No. 2767633-04-3
SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 value of 15 nM. As a guanine nucleotide exchange factor (GEF), SOS1 activates KRAS by facilitating the conversion of GDP to GTP. SOS1-IN-21 demonstrates potent antiproliferative activity, with IC50 values of 16 nM for NCI-H358 cells and 17 nM for Mia Paca-2 cells. It exhibits significant antitumor activity in Mia Paca-2 xenograft models and is useful for researching KRAS-mutated tumors, such as pancreatic cancer.
SOS1-IN-21
Copy Product Info😃Good
Catalog No. T212275Cas No. 2767633-04-3
SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 value of 15 nM. As a guanine nucleotide exchange factor (GEF), SOS1 activates KRAS by facilitating the conversion of GDP to GTP. SOS1-IN-21 demonstrates potent antiproliferative activity, with IC50 values of 16 nM for NCI-H358 cells and 17 nM for Mia Paca-2 cells. It exhibits significant antitumor activity in Mia Paca-2 xenograft models and is useful for researching KRAS-mutated tumors, such as pancreatic cancer.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 value of 15 nM. As a guanine nucleotide exchange factor (GEF), SOS1 activates KRAS by facilitating the conversion of GDP to GTP. SOS1-IN-21 demonstrates potent antiproliferative activity, with IC50 values of 16 nM for NCI-H358 cells and 17 nM for Mia Paca-2 cells. It exhibits significant antitumor activity in Mia Paca-2 xenograft models and is useful for researching KRAS-mutated tumors, such as pancreatic cancer. |
| In vitro | SOS1-IN-21 (Compound 21), when used in concentrations ranging from 0 to 3000 nM, significantly enhances the growth inhibitory effect on Mia PaCa-2 cells when combined with the KRASG12C inhibitor AMG510. |
| In vivo | Administered twice daily for 23 days at a dosage of 12-25 mg/kg orally, SOS1-IN-21 (Compound 21) significantly inhibited tumor growth in the Mia PaCa-2 xenograft model and demonstrated enhanced efficacy when combined with AMG510. |
| Molecular Weight | 493.52 |
| Formula | C25H30F3N3O4 |
| Cas No. | 2767633-04-3 |
| Smiles | N([C@H](C)C1=C(F)C(C(C(C)(C)O)(F)F)=CC=C1)C=2C3=C(C=C(OC)C(OCCOC)=C3)N=C(C)N2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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