SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).

the BCR-ABL protein levels in a concentration dependent manner significantly reduced by SIAIS178 (1-100 nM; for 16 hours) . SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5. in BCR-ABL driven CML cell lines, SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.

Tumor progression in a dose-dependent manner attenuated by SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days), as determined by serial volumetric measurement . SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.

2376047-73-1

C50H62ClN11O6S2

1012.68

DMSO:300 mg/mL (296.24 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years