SOS1 Degrader

BTX-6654 formate is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 formate reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.

PROTAC SOS1 degrader-1 TFA is a degrader of SOS1 PROTAC, with a DC₅₀ of 98.4 nM and a K_d value of 44 nM. PROTAC SOS1 degrader-1 TFA induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 TFA reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 TFA inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 TFA can be used for the research of KRAS-driven cancers.

BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.

PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC₅₀ of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC₅₀ of 5 nM.

PROTAC SOS1 degrader-7 (Example 15) is a SOS1 PROTAC degrader. PROTAC SOS1 degrader-7 has anti-tumor activity . (Pink: SOS1 ligand (HY-163583); Black: linker (HY-163584); Blue: E3 ligase ligand (HY-W454906)).

PROTAC SOS1 degrader-4 (Compound 10) is a PROTAC degrader that targets the SOS1 protein for degradation by recruiting cereblon. It degrades SOS1 in NCI-H358, A-427, SW-620, and DLD-1 cells and inhibits the proliferation of various KRAS-mutant tumor cells, making it a useful tool for cancer research.

PROTAC SOS1 degrader-9 (Compound 10) is a SOS1 PROTAC degrader. PROTAC SOS1 degrader-9 can be used in cancer research.

(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo.

PROTAC SOS1 degrader-3 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-3 effectively targeted SOS1 for degradation through the ubiquitin-proteasome system.

PROTAC SOS1 degrader-8 (Compound 1) is a SOS1 PROTAC degrader. PROTAC SOS1 degrader-8 can be used in cancer research.

PROTAC SOS1 degrader-1 is a degrader of SOS1 PROTAC, with a DC₅₀ of 98.4 nM and a K_d value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers.

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a K_d of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRAS^G12C or KRAS^G12D to SOS1, with the IC₅₀ values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity.