For research use only. Not for therapeutic Use.
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13[1].2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46[1].82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research[1].
| Catalog Number | I040323 |
| Synonyms | N-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]-4-[2-[5-methoxy-N-methyl-4-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-2-(prop-2-enoylamino)anilino]ethyl-prop-2-ynylamino]butanamide;2,2,2-trifluoroacetic acid |
| Molecular Formula | C50H50F6N10O10 |
| Purity | ≥95% |
| InChI | InChI=1S/C46H48N10O6.2C2HF3O2/c1-6-21-55(22-11-16-42(58)48-33-14-10-13-30-32(33)28-56(45(30)61)38-17-18-43(59)52-44(38)60)24-23-53(3)39-26-40(62-5)36(25-35(39)49-41(57)7-2)51-46-47-20-19-34(50-46)31-27-54(4)37-15-9-8-12-29(31)37;2*3-2(4,5)1(6)7/h1,7-10,12-15,19-20,25-27,38H,2,11,16-18,21-24,28H2,3-5H3,(H,48,58)(H,49,57)(H,47,50,51)(H,52,59,60);2*(H,6,7) |
| InChIKey | NMZXAPUYEVNTCV-UHFFFAOYSA-N |
| SMILES | CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(CCCC(=O)NC5=CC=CC6=C5CN(C6=O)C7CCC(=O)NC7=O)CC#C)OC.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O |
| Reference | [1]. Zhang W, et al. Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo. Eur J Med Chem. 2022 Aug 5;238:114509. |
