kras-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.

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-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/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.

BI1701963 is an orally effective inhibitor that targets the SOS1 and KRAS interaction, specifically inhibiting the activation of KRAS by blocking its GTP loading. This compound is utilized in cancer research to explore potential therapeutic effects against KRAS-driven malignancies.

ZZ151 is an effective and selective SOS1 PROTAC with in vivo anti-tumor efficacy against KRAS-mutant cancers. This compound induces rapid and specific degradation of SOS1 and exhibits strong anti-proliferative activity against a wide range of KRAS mutation-driven cancer cells. In murine xenograft models with KRASG12D and G12V mutations, ZZ151 demonstrates superior anticancer activity. It represents a promising lead compound for developing new chemotherapeutic agents targeting KRAS mutations.

BTX-6654 is a cereblon-based bifunctional SOS1 PROTAC degrader. This compound exhibits antiproliferative activity against cells with various KRAS mutations by reducing the expression of downstream signaling markers pERK and pS6.

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.

SOF-436 is a KRAS inhibitor that can suppress SOS1-mediated KRAS nucleotide exchange (IC50 = 60 μM) and inhibit the interaction between KRAS and the effector protein RAF. SOF-436 is applicable to cancer research.

BTX-7312 is a cereblon-based SOS1 bifunctional degrader and acts as a molecular glue (molecular glue). It reduces downstream signaling markers pERK and pS6 and demonstrates antiproliferative activity in cells with various KRAS mutations.

KRAS ligand 4 (Compound 2) is a dual-functional molecular glue degrader based on SOS1. It reduces downstream signaling markers pERK and pS6, and exhibits antiproliferative activity in cells with various KRAS mutations.

LHF418 is a potent SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells. It effectively inhibits RAS signaling and colony formation in KRAS-driven cancer cells.

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.

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

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

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.

KRAS G12C inhibitor 25 is an inhibitor of KRAS G12C. KRAS G12C inhibitor 25 inhibits the SOS1-assisted GDP/GTP exchange activity of KRAS-G12C mutants with an IC50 value of 0.48 nM.

BI-0474 is a potent KRASG12C inhibitor that inhibits GDP-KRAS::SOS1 protein-protein interactions with an IC50 value of 7.0 nM.BI-0474 exhibits significant antiproliferative activity against NCI-H358 cells harboring the G12C mutation, and shows significant anti-tumor activity in a non-small cell lung cancer xenograft model. activity.BI-0474 can be used for cancer research.

KRAS G12C inhibitor 56, a powerful inhibitor of SOS1 with an inhibitory concentration (IC50) of 1.6 nM, holds promise for use in cancer research.

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].

SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity ( EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS [1] .