CH091138
CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand ; Blue: VHL E3 ligase ligand (HY-138678) ; Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B) ).
Product Specifications
UNSPSC
12352005
Target
Apoptosis; PROTACs; Ras
Related Pathways
Apoptosis; GPCR/G Protein; MAPK/ERK Pathway; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
Molecular Formula
C59H69FN10O6S
Molecular Weight
1065.31
References & Citations
[1]Jeon E, et al. KRASG12D selective VHL-PROTAC with sparing KRASWT and other KRAS mutants. Eur J Med Chem. 2025 Jul 5;297:117928.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
K-Ras; von Hippel-Lindau (VHL)
Frequently Asked Questions
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