MS 39 - CAS 2675490-92-1

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively) . However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

Others, EGFR, PROTACs

PROTAC, Others, Tyrosine Kinase/Adaptors, JAK/STAT signaling, Angiogenesis

2675397

C55H71ClFN9O7S

1056.72

N(C=1C2=C(C=C(OC)C(OCCCN3CCN(C(CCCCCCCCCC(N[C@H](C(=O)N4[C@H](C(NCC5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)[C@@](C)(C)C)=O)=O)CC3)=C2)N=CN1)C7=CC(Cl)=C(F)C=C7

-20°C

Ice Packs

PROTAC