Chemical Name: (R)-6,7-Dimethoxy-2-methyl-N-[1-[4-[2-[(methylamino)methyl]phenyl]thiophene-2-yl]ethyl]quinazolin-4-amine
Biological ActivityPotent KRas/son of sevenless 1 (SOS1) interaction inhibitor (IC50 = 21 nM); active R-enantiomer. Downregulates active RAS in tumor cells. Inhibits RAS-RAF-MEK-ERK pathway. Exhibits synergistic effects with KRASG12C inhibitor ARS-853.
Negative control also available.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Hillig et al.
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