3097564-20-7
Chemical Structure
PROTAC BET Degrader-18
- CAS No.: 3097564-20-7
- Formula:C51H58N8O11S
- Molecular Weight:991.12
InChIKey: AXRFJFBHXWNBQT-UHFFFAOYSA-N
SMILES: CC(C1=C(NC(C(NC2=C(C=CC(S(=O)(N3CCOCC3)=O)=C2)OCCCC(N4CCN(CC4)CC5CCN(CC5)C6=CC=C7C(N(C(C7=C6)=O)C8CCC(NC8=O)=O)=O)=O)=O)=C1C9=CC=CC=C9)C)=O
Biological Activity: PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer[1].
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PROTAC BET Degrader-18 | PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer. | |||||||||||||||||||||
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