SIAIS562055
SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638) ; Black: linker (HY-W539874) ; Blue: E3 ligase ligand (HY-W076696) ) [1].
Product Specifications
UNSPSC
12352211
Target
PROTACs; Ras; SOS1
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/siais562055.html
Smiles
COC1=CC2=C(C(N[C@@H](C3=CC(N)=CC(C(F)(F)F)=C3)C)=NC(C)=N2)C=C1OC4CCN(CC4)CCCCCCCCCCCCSC5=C6C(C(N(C6)C7C(NC(CC7)=O)=O)=O)=CC=C5
Molecular Formula
C49H62F3N7O5S
Molecular Weight
918.12
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon; K-Ras
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