产品
编 号：F756796
分子式：C63H75ClN12O7S
分子量：1179.86
分子式：C63H75ClN12O7S
分子量：1179.86
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CAS No: 2913177-53-2
产品详情
生物活性：
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.
体外研究：
YF135 inhibits the proliferation of H358 and H23 cells with IC50 values of 153.9 and 243.9 nM, respectively.YF135 obviously decreases the protein level of KRASG12C and phospho-ERK in H358 and H23 cells in a time (3 μM, 0-36 h) and dose (0-10 μM, 24 h) dependent manner, while the washout by fresh medium significantly rescues such effects.YF135 induces degradation of KRASG12C through the E3 ligase VHL mediated proteasome pathway. YF135 covalently bind to KRASG12C and VHL ligase to form a ternary complex.
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.
体外研究：
YF135 inhibits the proliferation of H358 and H23 cells with IC50 values of 153.9 and 243.9 nM, respectively.YF135 obviously decreases the protein level of KRASG12C and phospho-ERK in H358 and H23 cells in a time (3 μM, 0-36 h) and dose (0-10 μM, 24 h) dependent manner, while the washout by fresh medium significantly rescues such effects.YF135 induces degradation of KRASG12C through the E3 ligase VHL mediated proteasome pathway. YF135 covalently bind to KRASG12C and VHL ligase to form a ternary complex.
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