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SOS1-IN-21
🥰Excellent
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
🥰Excellent
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.
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| 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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For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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