sos1

SOS1-IN-15 is an orally active and potent SOS1 inhibitor with potential antitumor activity.SOS1-IN-15 is used in the study of colon cancer.

BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).

RMC-0331 (RM-023) is an orally available and potent SOS1 inhibitor with potential anticancer activity, blocking RAS activation by disrupting RAS-SOS1 interactions.

I-49 free base (Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]-6-(tetrahydro-2H-pyran-4-yl)-) is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.

MRTX0902 is an effective and high selective inhibitor of SOS1 with an IC50 of 46 nM and a Ki of 2 nM.

SOS1 EGFR-IN-2 (Compound 4) functions as a dual inhibitor of SOS1 and EGFR, exhibiting IC50 values of 8.3 and 14.6 nM, respectively. It demonstrates significant antiproliferative effects on cancer cells harboring various KRAS mutations.

SOS1-IN-17 (Compound 8d) is an orally active inhibitor targeting the SOS1-KRASG12C interaction, with an IC50 of 5.1 nM. It suppresses ERK phosphorylation in DLD-1 cells with an IC50 of 18 nM and demonstrates antiproliferative activity in KRASG12C-mutant Mia-Paca-2 cells, with an IC50 of 0.11 μM. In mouse models, SOS1-IN-17 shows antitumor efficacy against pancreatic cancer.

SOS1 activator 2 (Compound 65) is a benzothiazole derivative and an activator of SOS1. It demonstrates a high binding affinity for SOS1, with a Kd of 9 nM. By modulating the Ras-ERK signaling pathway, SOS1 activator 2 is suitable for tumor research.

SOS1-IN-18 (Compound 8) is an inhibitor of the Son of Sevenless 1 protein (SOS1) with a dissociation constant (KD) of 2.6 nM. It disrupts the SOS1-KRAS G12C interaction with an IC50 of 3.4 nM, inhibits ERK phosphorylation in H358 cells with an IC50 of 31 nM, and curtails the proliferation of H358 cells with an IC50 of 5 nM.

SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 nM).

SOS1-IN-3 is an effective inhibitor of SOS1 (son of sevenless homolog 1) (IC50=5 nM). SOS1-IN-3 shows antitumor activity.

SOS1-IN-13 is a potent inhibitor of son of sevenless homolog 1 (SOS1), displaying IC50 values of 6.5 nM for SOS1 and 327 nM for pERK. SOS1-IN-13 holds significant research value in anticancer studies.

SOS1-IN-12 is a potent inhibitor of SOS1, with a Ki of 0.11 nM, and exhibits an IC50 of 47 nM on pERK.

SOS1-IN-9 is a potent inhibitor of SOS1 that targets KRAS G12C-SOS1 with an IC50 of 116.5 nM.

SOS1-IN-10 is a potent inhibitor of SOS1, targeting KRAS G12C-SOS1 with an IC50 of 13 nM.

SOS1-IN-7 (compound 18-p1) is a potent SOS1 inhibitor with IC50 values of 20 nM for SOS1-G12D and 67 nM for SOS1-G12V.

SOS1-IN-6 (compound 33-P1) is a potent inhibitor of SOS1, exhibiting an IC50 of 14.9 nM on SOS1-G12D and 73.3 nM on SOS1-G12V.

SOS1-IN-4 is a potent inhibitor of SOS1 (IC50: 56 nM) and can be used to study KRAS-C12C SOS1 interactions.

SOS1-IN-8 is an inhibitor of SOS1 and acts on SOS1-G12D (IC50: 11.6 nM) and SOS1-G12V (IC50: 40.7 nM).

SOS1 activator 1 is an activator of SOS1-mediated nucleotide exchange (Kd: 44 nM).SOS1 is a guanine nucleotide exchange factor that binds to Ras proteins and catalyzes the exchange of GDP for GTP on RAS, resulting in the exchange of GDP originally bound to Ras for GTP.

SOS1-IN-5 is a pyrimidine bicyclic derivative and a potent inhibitor of SOS1. SOS1-IN-5 interferes with the RAS-SOS1 interaction, thereby blocking KRAS activation and exhibiting broad-spectrum inhibition of KRAS activity. compound 4).

SOS1-IN-14 is a selective, potent, orally active SOS1 inhibitor (IC50: 3.9 nM). sOS1-IN-14 is absorbed in the intestine using a P-glycoprotein-mediated efflux mechanism. sOS1-IN-14 can be used in the study of KRAS mutated cancers and is more effective in tumour suppression than BI-3406.

PROTAC SOS1 degrader-2, a potent degrader of PROTAC SOS1, effectively reduces the expression of pERK and RAS-GTP in a dose-dependent manner. It significantly inhibits tumor growth in vivo [1].

PROTAC SOS1 degrader-1, a potent compound, demonstrates an effective degradation of PROTAC SOS1 with a DC50 value of 98.4 nM. It exhibits antiproliferative activity against cancer cells harboring diverse KRAS mutations and has shown an antitumor effect with low toxicity [1].