Catalog No.: PC-27137Not For Human Use, Lab Use Only.
XYD113 is a potent and highly selective, orally bioavailable CRBN-dependent GSPT1 molecular glue degrader, exerts potent antiproliferative activity against 22Rv1 cells with IC50 of 69 nM, induces complete degradation of GSPT1 at 111 nM.
XYD113 is a potent and highly selective, orally bioavailable CRBN-dependent GSPT1molecular glue degrader, exerts potent antiproliferative activity against 22Rv1 cells with IC50 of 69 nM, induces complete degradation of GSPT1 at 111 nM.
XYD113 exhibits significant antiproliferative activity (IC50 < 100 nM) against multiple MYC-overexpressing cancer cell lines (22Rv1, MV4-11, MOLM-16, Calu-1, HS-SY-II), and induces GSPT1 degradation in a dose- and time-dependent manner.
XYD113 at 1 uM for 6 h led to a complete degradation of GSPT1 in 22Rv1 cells.
XYD113 shows exceptional selectivity over SALL4, IKZF1/2/3, ZFP91, or CK1α.
XYD113 functions as a molecular glue to facilitate the formation of the CRBN-GSPT1 ternary complex, a rate-limiting step in targeted protein degradation via the UPS.
XYD113 (5 mg/kg, oral) suppresses tumor growth in a 22Rv1 xenograft model with a favorable safety profile.
