OPN-9652 [CAS 2866423-35-8]

OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61) . OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research[1].

[2866423-35-8]

C19H15F4NO2

365.32

C=CC(N1CC2=C(C=CC(OC3=CC=C(C(F)(F)F)C(F)=C3)=C2)CC1)=O

YAP

TEAD

Room temperature