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.

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

SOS1-IN-1 is an inhibitor of SOS1.

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

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 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.

PROTACSOS1 degrader-6 (compound 23) is an effective degrader of SOS1 PROTACs and works synergistically with KRASG12C inhibitors.

SOS1 Ligand intermediate-3 (Compound 5) is an SOS1 binder used in the synthesis of SOS1PROTACs in combination with pomalidomide.

SOS1 Ligand intermediate-5 is a ligand for son of sevenless 1 (SOS1) and is utilized in the synthesis of PROTAC SOS1 degrader-10.

SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for prostate cancer, effectively suppressing downstream effector molecules through the inhibition of SOS1 and EGFR. It induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. In prostate cancer cells PC-3, it demonstrates significant antitumor activity with an IC50 of 0.45±0.03 μM.

PROTACSOS1 degrader-10 (Compound 11o) is a degrader of son of sevenless 1 (SOS1) that functions through CRBN- and protease-dependent mechanisms. It effectively degrades SOS1 in KRAS-mutated cancer cells SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. Additionally, PROTACSOS1 degrader-10 inhibits the proliferation of SW620, A549, and DLD-1 cells, with IC50 values of 36.7, 52.2, and 107 nM, and suppresses ERK phosphorylation.

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.

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].

PROTAC SOS1 Degrader-3 is a potent agent specifically designed to target and degrade SOS1 via the ubiquitin-proteasome system [1].

PROTAC SOS1 Degrader-4 (compound 10) is a potent degrader of SOS1 and exhibits antiproliferative activity [1].

SOS1/KRAS-IN-1 (Compound 2) serves as an inhibitor of SOS1/KRAS, with potential application in the study of diseases mediated by SOS1/KRAS [1].

SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 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-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-19 (Compound 10i) is a potent inhibitor of SOS1 (Son of Sevenless 1) with an IC50 value of 165.2 nM. It functions by blocking the GDP/GTP exchange in the KRAS signaling pathway, thereby inhibiting KRAS activation. SOS1-IN-19 shows potential for research in cancers driven by KRAS, such as non-small cell lung cancer and colorectal cancer.

SOS1-IN-20 (Compound 12f) is an orally active inhibitor of SOS1, exhibiting an IC50 of 5.11 nM against KRASG12C::SOS1. It prevents KRAS activation and its downstream signaling by disrupting the KRAS-SOS1 interaction. In PC-9 cells, it shows an IC50 of 253 nM for p-ERK, while its IC50 for the hERG channel is 16.71 μM. SOS1-IN-20 also inhibits tumor cell proliferation, displaying antitumor activity.