SCH-1473759 hydrochloride是一种多靶点极光激酶抑制剂，对极光激酶A和B的IC50值分别为 4 和13 nM。

SCH-1473759 hydrochloride is an inhibitor of aurora(aurora A and B with IC50s of 4 and 13 nM, respectively).

SCH-1473759 directly binds to aurora A and B(Kds of 20 and 30 nM, respectively), also inhibits the Src family of kinases with IC50 less than 10 nM, Chk1 with IC50 of 13 nM, VEGFR2 with IC50 of 1 nM), and IRAK4 with IC50 of 37 nM. SCH 1473759 inhibits tumor cell lines from different tissues (breast, ovarian, prostate, lung, colon, brain, gastric, renal, skin, and leukemia). The most sensitive cell lines includ A2780, LNCap, N87, Molt4, K562, and CCRF-CEM with IC50 values<5 nM[2].

SCH-1473759(5 mg/kg ,ip, bid) was well tolerated in the continuous dosing regimen and showed 50% tumor growth inhibition (TGI) on day 16. SCH-1473759(10mg/kg,ip, bid) is well-tolerated in an intermittent schedule (5 days on, 5 days off) and gave 69% TGI on day 16. SCH-1473759 showed good exposure in all species, with high clearance rates in rodents and moderate clearance rates in dogs and monkeys.The half-life is also moderate, but the tissue distribution is high[1]. SCH 1473759 dose- and schedule-dependent anti-tumor activity in four human tumor xenograft models. Further, the efficacy is enhanced in combination with taxanes and found to be most efficacious when SCH 1473759 is dosed 12-h post-taxane treatment[2].

1094067-13-6

C20H27ClN8OS

463.0

DMSO:70 mg/mL (151.19 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years