产品
编 号：F753824
分子式：C39H38N6O9S
分子量：766.82
分子式：C39H38N6O9S
分子量：766.82
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CAS No: 2570470-42-5
产品详情
生物活性：
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
体外研究：
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8?hours) shows anti-proliferation activity with IC50 value of 12.25?nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8?h in MV4-11 cells.PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8?hours) shows anti-proliferation activity with IC50 value of 12.25?nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8?h in MV4-11 cells.PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines.PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI50 values of the three leukemia cell lines were lower than 50?nM, consistent with the activity of leukemia MV4-11 cells.PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC50: 0.081?μM), colon cancer (colo-205 IC50: 0.1557?μM) and thyroid cancer(TT IC50: 0.037451?μM).
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
体外研究：
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8?hours) shows anti-proliferation activity with IC50 value of 12.25?nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8?h in MV4-11 cells.PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8?hours) shows anti-proliferation activity with IC50 value of 12.25?nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8?h in MV4-11 cells.PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines.PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI50 values of the three leukemia cell lines were lower than 50?nM, consistent with the activity of leukemia MV4-11 cells.PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC50: 0.081?μM), colon cancer (colo-205 IC50: 0.1557?μM) and thyroid cancer(TT IC50: 0.037451?μM).
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