2913176-81-3
Chemical Structure
(4S)-PROTAC SOS1 degrader-1
- CAS No.: 2913176-81-3
- Formula:C57H76ClFN10O4S
- Molecular Weight:1051.79
IUPAC Name: 3-bromo-6,7-dihydro-5H-cyclopenta[b]pyridin-5-amine
InChIKey: AZBRWXRYNYEDKG-UZBSLLNPSA-N
SMILES: O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](O)C[C@H]1C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)CCCCCCCCN4CCN(CC4)C5=C6N=C(N7CC8(CNC8)C7)N(CC9=CC(C)=C(F)C(C)=C9)C6=CC(Cl)=C5
Biological Activity: (4S)-PROTAC SOS1 degrader-1 is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd 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[1].
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(4S)-PROTAC SOS1 degrader-1 | (4S)-PROTAC SOS1 degrader-1 is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd 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. | |||||||||||||||||||||
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