For research use only. Not for therapeutic Use.
PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878))[1].
PRO-6E (0.03-10 μM; 48 h) inhibits the cell growth in MKN-45, SNU-638 cells[1].
PRO‐6 E (1 μM; over 24 h) facilitates MET degradation in MKN-45 cells[1].
PRO‐6 E (0.1-1 μM; 48 h) increase in the percentage of G2/M phase cells and decrease in the percentage of S phase cells in MKN-45 cells[1].
PRO-6E (oral gavage; 30 mg/kg/day for 15 days) inhibits tumor growth in MKN‐45 cell‐derived xenograft tumor model[1].
| Catalog Number | I040070 |
| CAS Number | 2353493-69-1 |
| Synonyms | 4-[8-[4-[4-[6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyridin-3-yl]pyrazol-1-yl]piperidin-1-yl]-8-oxooctoxy]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione |
| Molecular Formula | C42H44Cl2FN7O7 |
| Purity | ≥95% |
| InChI | InChI=1S/C42H44Cl2FN7O7/c1-24(36-29(43)11-12-30(45)38(36)44)59-33-20-25(21-47-39(33)46)26-22-48-51(23-26)27-15-17-50(18-16-27)35(54)10-5-3-2-4-6-19-58-32-9-7-8-28-37(32)42(57)52(41(28)56)31-13-14-34(53)49-40(31)55/h7-9,11-12,20-24,27,31H,2-6,10,13-19H2,1H3,(H2,46,47)(H,49,53,55)/t24-,31?/m1/s1 |
| InChIKey | JSQFSAUVTNADLF-LZDHLTRGSA-N |
| SMILES | CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCN(CC4)C(=O)CCCCCCCOC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)N |
| Reference | [1]. Chen JJ, et al. Crizotinib-based proteolysis targeting chimera suppresses gastric cancer by promoting MET degradation. Cancer Sci. 2023;114(5):1958-1971. |
