SOS1 Inhibitor

SOS1-IN-2 (Compound 1-1) is an inhibitor of SOS1 with an IC₅₀ value of 5 nM. SOS1-IN-2 can be used in tumor research.

KRAS-IN-62 is an orally effective pan-KRAS inhibitor that potently inhibits SOS1-mediated KRAS nucleotide exchange (IC₅₀ < 10 nM for KRAS G12D/G12V/G12C/WT). KRAS-IN-62 inhibits pERK signaling and cell proliferation in KRAS-mutant tumor cells (pERK IC₉₀ = 0.51 nM in GP2D cells). KRAS-IN-62 inhibits tumor growth in vivo, with plasma concentrations exceeding IC₅₀ for ~20 h after oral administration in beagle dogs. KRAS-IN-62 can be used in studies of KRAS mutation-related cancers, such as colorectal cancer.

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

SOS1-IN-5 is a potent inhibitor of SOS1. SOS1-IN-5 is a pyrimidobicyclic derivative. SOS1-IN-5 blocks the activation of KRAS by interfering with RAS-SOS1 interaction, and achieves the purpose of broad-spectrum inhibition of KRAS activity. SOS1-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2021203768A1, compound 4).

SOS1/KRAS-IN-1(Compound 2) is a SOS1/KRAS inhibitor, which can be used in the research of SOS1/KRAS-mediated diseases.

SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC₅₀s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants.

PROTAC SOS1 degrader-10 is a SOS1 PROTAC degrader dependent on CRBN and the proteasome. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS-mutant cancer cells SW620, A549 and DLD-1, with DC₅₀ values of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits ERK phosphorylation. PROTAC SOS1 degrader-10 suppresses the proliferation of KRAS-mutant cancer cells via antiproliferative activity. PROTAC SOS1 degrader-10 can be used in studies related to KRAS-mutant cancers.

VUBI1-octanoic acid is a conjugate of SOS1 ligand and linker, which can be used in the synthesis of (4S)-PROTAC SOS1 degrader-1 (HY-144657).

SOS1-IN-9 is a potent SOS1 inhibitor with an IC₅₀ of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302).

SL43 is an orally active and potent SOS1 inhibitor with a K_d of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model.

SOS1-IN-6 (compound 33-P1) is a potent SOS1 inhibitor with IC₅₀s of 14.9 and 73.3 nM for SOS1-G12D and SOS1-G12V, respectively.

SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC₅₀ of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC₅₀ values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer.

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.

SOS1 Ligand intermediate-7 (65) is an intermediate for the synthesis of SOS1 ligand (HY-111671). SOS1 activator 1 (HY-111671) can be used for the synthesis of PROTAC SOS1 degrader-1 (HY-145737).

SOS1-IN-13 is a potent son of sevenless homolog 1 (SOS1) inhibitor with IC₅₀s of 6.5 nM and 327 nM for SOS1 and pERK, respectively. SOS1-IN-13 can be used for researching anticancer.

KRAS ligand 4 (compound 2) is a bifunctional degrader based on SOS1. KRAS ligand 4 reduces downstream signaling markers pERK and pS6 and displays anti-additional activity in cells with multiple KRAS mutations.

VHL Ligand intermediate-2 (compound 18c) is an intermediate for the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs.

SOS1-IN-28 is an orally active, blood-brain barrier permeable SOS1 inhibitor with an IC₅₀ value of 0.11 μM. SOS1-IN-28 disrupts the SOS1: KRAS protein-protein interaction, with an IC₅₀ of 0.29 μM for the KRAS-RAF interaction. SOS1-IN-28 blocks GTP loading of KRAS, inhibits RAS-MAPK pathway activity, and reduces cancer cell proliferation. SOS1-IN-28 can be used for the research of KRAS^G12C-mutant lung cancer.

SOS1 Ligand intermediate-6 is an intermediate for the synthesis of SOS1 ligand and can be used to synthesize PROTACs.

Sos1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sos1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.