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 nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.
性状
Solid
IC50 & Target[1][2]
KRAS-SOS1 KRas G12C 140 nM (EC50)
体外研究(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 Colo320-HSR cells, are similarly affected.SAH-SOS1A TFA (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85D/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years;-20°C 1 ye