For research use only. Not for therapeutic Use.
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer[1].
MS9427 TFA has antiproliferative activity against HCC-827 cells, with a GI50 of 0.87 ± 0.27 μM[1].
MS9427 TFA (0-10 μM, 16 h) potently induces EGFRDel19 degradation (DC50=82 ± 73 nM) and inhibits EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells[1].
| Catalog Number | I041420 |
| Synonyms | 5-[2-[2-[2-[2-[2-[3-[4-[3-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypropyl]piperazin-1-yl]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione;2,2,2-trifluoroacetic acid |
| Molecular Formula | C50H59ClF4N8O14 |
| Purity | ≥95% |
| InChI | InChI=1S/C48H58ClFN8O12.C2HF3O2/c1-64-41-30-39-36(45(53-31-52-39)54-33-4-6-38(50)37(49)28-33)29-42(41)70-16-2-11-56-12-14-57(15-13-56)44(60)9-17-65-19-21-67-23-25-69-26-24-68-22-20-66-18-10-51-32-3-5-34-35(27-32)48(63)58(47(34)62)40-7-8-43(59)55-46(40)61;3-2(4,5)1(6)7/h3-6,27-31,40,51H,2,7-26H2,1H3,(H,52,53,54)(H,55,59,61);(H,6,7) |
| InChIKey | SZDKGDPFHUTOHP-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCN(CC4)C(=O)CCOCCOCCOCCOCCOCCNC5=CC6=C(C=C5)C(=O)N(C6=O)C7CCC(=O)NC7=O.C(=O)(C(F)(F)F)O |
| Reference | [1]. Yu X, et al. Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J Med Chem. 2022 Jun 23;65(12):8416-8443. |
