2913177-53-2
Chemical Structure
YF135
- CAS No.: 2913177-53-2
- Formula:C63H75ClN12O7S
- Molecular Weight:1179.86
IUPAC Name: 4,4,5,5-tetramethyl-2-(3-(2,2,2-trifluoroethyl)phenyl)-1,3,2-dioxaborolane
InChIKey: VJEBOMJUVXOGQI-ZAONMBGGSA-N
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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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Keywords
