YF135
YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway[1].
Product Specifications
CAS Number
2913177-53-2
UNSPSC
12352005
Target
PERK; PROTACs
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/yf135.html
Solubility
10 mM in DMSO
Smiles
CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCOCCCN4CCC[C@H]4COC5=NC6=C(C(N7CCN([C@H](C7)CC#N)C(/C(C#N)=C/C8CC8)=O)=N5)CCN(C6)C9=CC=CC%10=C9C(Cl)=CC=C%10)=O)=O)O)=O
Molecular Formula
C63H75ClN12O7S
Molecular Weight
1179.86
References & Citations
G12C
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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