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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity ( EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nuc
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IC50& Target:KRAS-SOS1 KRas G12C 140 nM (EC 50 ) KRas G12D 109 nM (EC 50 ) KRas G12V 154 nM (EC 50 ) KRas G12S 155 nM (EC 50 ) KRas Q61H 175 nM (EC 50 ) K-Ras WT 106 nM (EC 50 )
In Vitro:SAH-SOS1A TFA (0.625-40 μM; 24 hours) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo
In Vivo:SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85D V12 /ActinGS) treatment notably decreases the phosphorylation state of ERK1/2. MCE has not independently confirmed the accuracy of these methods. They are fo
Biological Activity:SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity ( EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nuc