2913185-35-8
Chemical Structure
PROTAC SOS1 degrader-1
- CAS No.: 2913185-35-8
- Formula:C57H76ClFN10O4S
- Molecular Weight:1051.79
IUPAC Name: tert-butyl (R)-(1-oxobutan-2-yl)carbamate
InChIKey: AZBRWXRYNYEDKG-VWELVXIZSA-N
SMILES: O=C([C@H]1N(C([C@@H](NC(CCCCCCCCN2CCN(C3=C4C(N(CC5=CC(C)=C(F)C(C)=C5)C(N6CC7(CNC7)C6)=N4)=CC(Cl)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C8=CC=C(C9=C(C)N=CS9)C=C8)C
Biological Activity: PROTAC SOS1 degrader-1 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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PROTAC SOS1 degrader-1 | PROTAC SOS1 degrader-1 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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