Bioactivity:

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

CAS nr:

2230821-27-7

Purity:

98%

Molecular Weight:

934,51

SMILES:

CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O

Formula:

C47H57ClFN7O8S

Pathway:

Tyrosine Kinase/Adaptors,Angiogenesis,JAK/STAT signaling

Target:

EGFR,EGFR,EGFR