3052745-16-8
Chemical Structure
PROTAC K-Ras Degrader-5
- CAS No.: 3052745-16-8
- Formula:C57H63F3N10O5
- Molecular Weight:1025.17
InChIKey: VUGUNNWXJMBUFV-OGFZEQTGSA-N
SMILES: C#CC1=C(C=CC2=CC(O)=CC(C3=C(C4=NC(OCCN5CCC(CC5)CC6CCN(CC6)CC7CCN(CC7)C8=CC=C9C(N(CC9=C8F)C%10CCC(NC%10=O)=O)=O)=NC(N%11C[C@H]%12N[C@H](CC%12)C%11)=C4C=N3)F)=C21)F
Biological Activity: PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer[1].
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PROTAC K-Ras Degrader-5 | 95.04% | PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer. | ||||||||||||||||||||
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