For research use only. Not for therapeutic Use.
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)[1].
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[1].
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[1].
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[1].
| Catalog Number | I043573 |
| CAS Number | 3032108-74-7 |
| Synonyms | 2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxy-N-[8-[[6-fluoro-2-[[(2-morpholin-4-yl-9-propan-2-ylpurin-6-yl)amino]methyl]-1H-benzimidazol-5-yl]amino]octyl]acetamide |
| Molecular Formula | C43H51FN12O7 |
| Purity | ≥95% |
| InChI | InChI=1S/C43H51FN12O7/c1-25(2)55-24-48-37-38(52-43(53-39(37)55)54-16-18-62-19-17-54)47-22-33-49-29-20-27(44)28(21-30(29)50-33)45-14-7-5-3-4-6-8-15-46-35(58)23-63-32-11-9-10-26-36(32)42(61)56(41(26)60)31-12-13-34(57)51-40(31)59/h9-11,20-21,24-25,31,45H,3-8,12-19,22-23H2,1-2H3,(H,46,58)(H,49,50)(H,47,52,53)(H,51,57,59) |
| InChIKey | XZMGOWQHLJWQJN-UHFFFAOYSA-N |
| SMILES | CC(C)N1C=NC2=C(N=C(N=C21)N3CCOCC3)NCC4=NC5=CC(=C(C=C5N4)F)NCCCCCCCCNC(=O)COC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O |
| Reference | [1]. Tian Niu, et al. Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor. Eur J Med Chem. 2022 Jan 15;228:114012. |
