sos 1

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).

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.

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-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.

SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 value of 15 nM. As a guanine nucleotide exchange factor (GEF), SOS1 activates KRAS by facilitating the conversion of GDP to GTP. SOS1-IN-21 demonstrates potent antiproliferative activity, with IC50 values of 16 nM for NCI-H358 cells and 17 nM for Mia Paca-2 cells. It exhibits significant antitumor activity in Mia Paca-2 xenograft models and is useful for researching KRAS-mutated tumors, such as pancreatic cancer.

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).