SOS1-IN-21
SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 2767633-04-3
- Formula: C25H30F3N3O4
- Molecular Weight:493.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
| Species | Dose | Route | Tmax | Cmax | AUC0-t | T1/2 |
|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 0.94 h | 2200 ng/mL | 5831 ng·h/mL | 1.82 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mia PaCa-2 tumor cells induced xenograft model established in BALB/c nude mice[1]
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Dosage:12 mg/kg (Day 0-9) and 50 mg/kg (Day 9-23)
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Administration:Oral administration (p.o.), for 23 days
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Result:Showed a tumor inhibition rate of 38% at the end of the 23-day.
Resulted in a synergistic effect on tumor cell growth inhibition with AMG510.
Chemical Information
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CAS No. 2767633-04-3
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Molecular Weight 493.52
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Formula C25H30F3N3O4
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SMILES
CC(O)(C)C(F)(F)C1=CC=CC([C@H](NC2=C3C=C(OCCOC)C(OC)=CC3=NC(C)=N2)C)=C1F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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