(R, R) -Bexobrutideg [CAS 2649400-33-7]

(R, R) -Bexobrutideg is the (R, R) -enantiomer of Bexobrutideg. Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324) ; Blue: CRBN ligand (HY-171893) ; Black: linker)[2][3].

[2649400-33-7]

C42H54N12O5

806.96

NC(C1=C(N=C(N2C[C@H](N3C(N(CC3)C)=O)CCC2)C=N1)NC4=CC=C(C5CCN(CC5)CC6CCN(C7=CN=C(C(N[C@H]8C(NC(CC8)=O)=O)=O)C=C7)CC6)C=C4)=O

Btk; Drug Isomer; PROTACs

98.83

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature