2. MAPK/ERK Pathway
  3. SOS1
  4. 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.

SOS1-IN-21

SOS1-IN-21 Chemical Structure

CAS No. : 2767633-04-3

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SOS1-IN-21 Related Antibodies

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Description

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[1].

In Vitro

SOS1-IN-21 (Compound 21) (0-3000 nM) significantly enhances growth suppression in Mia PaCa-2 cells in combination of the KRASG12C inhibitor AMG510 (HY-114277)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SOS1-IN-21 Related Antibodies
In Vivo

SOS1-IN-21 (Compound 21) (12-50 mg/kg, p.o., twice daily, for 23 days) significantly inhibits tumor growth and the effect is enhanced with AMG510 in Mia PaCa-2 xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mia PaCa-2 tumor cells induced xenograft model established in BALB/c nude mice[1]
Dosage: 12 mg/kg (Day 0-9) and 50 mg/kg (Day 9-23)
Administration: Oral administration (p.o.), for 23 days
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.
Molecular Weight

493.52

Formula

C25H30F3N3O4
CAS No.
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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SOS1-IN-21 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SOS1-IN-212767633-04-3SOS1Ras/Rac guanine nucleotide exchange factor 1AntitumorKRAS mutationAcquired resistanceNCI-H358 cellsMia Paca-2 cellsxenograft mice modelInhibitorinhibitorinhibit

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