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.

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

SOS1-IN-1 is an inhibitor of SOS1.

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.

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].

PROTAC SOS1 degrader-5 (compound 4) serves as an effective degrader of PROTAC SOS1, exhibiting a DC50 of 13 nM. It robustly suppresses the proliferation of NCI-H358 cells, with an IC50 value of 5 nM [1].

PROTA CSOS1 degrader-8 (Compd 1) acts as a PROTAC degrader targeting SOS1.

PROTACSOS1 degrader-8 (Compd 10) is a PROTAC that targets the degradation of SOS1, featuring color-coded components.

PROTACSOS1 degrader-7 (Example 15) is a SOS1 PROTAC degrader with specific antitumor activity.