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编 号:F762972
分子式:C43H51FN12O7
分子量:866.94
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10mM*1mL in DMSO
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1mg
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生物活性:
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).

体外研究:
PP-C8 (0-30 μM; 24 hours; Bel-7402 and MDA-MB-231 cells) is a potent and highly selective CDK12-Cyclin K complex degrade.PP-C8 (0-3 μM; 24 hours; Bel-7402 and MDA-MB-231 cells) mediated CDK12-CycK complex degradation is cereblon and UPS dependent PROTAC-MOA.PP-C8 (0-3 μM; Bel-7402 and MDA-MB-231 cell lines) induces CDK12-Cyclin K degradation demonstrates superior synergistic antiproliferative activity with the PARP inhibition.
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