1094067-13-6
中文名称 | 1094067-13-6 |
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中文同义词 | AURORA A和AURORA B抑制剂(SCH-1473759 HYDROCHLORIDE);化合物SCH-1473759 HYDROCHLORIDE;2-(乙基((5-((6-甲基-3-(1H-吡唑-4-基)咪唑并[1,2-A]吡嗪-8-基)氨基)异噻唑-3-基)甲基)氨基)-2-甲基丙-1-醇X盐酸盐 |
英文名称 | SCH1473759 (HCl salt) |
英文同义词 | SCH1473759 (HCl salt);SCH-1473759 hydrochloride;SCH-1473759 HCl;Aurora Kinase,inhibit,SCH1473759,Inhibitor,SCH 1473759,SCH1473759 hydrochloride,SCH 1473759 hydrochloride,SCH-1473759 |
CAS号 | 1094067-13-6 |
分子式 | C20H27ClN8OS |
分子量 | 463 |
EINECS号 | |
相关类别 | 细胞生物学试剂;对照品 |
Mol文件 | 1094067-13-6.mol |
结构式 |
1094067-13-6 性质
储存条件 | Store at -20°C |
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溶解度 | 二甲基亚砜:70 mg/mL(151.19 mM) |
形态 | 固体 |
颜色 | 白色至黄色 |
Aurora A 4 nM (IC 50 ) |
Aurora B 13 nM (IC 50 ) |
SCH-1473759 directly binds to aurora A and B with K d s of 20 and 30 nM, respectively. SCH-1473759 also inhibits the Src family of kinases (IC 50 <10 nM), Chk1 (IC 50 =13 nM), VEGFR2 (IC 50 =1 nM), and IRAK4 (IC 50 =37 nM). It does not have significant activity (IC 50 >1000 nM) against 34 other kinases representing different families of the kinome. SCH-1473759 inhibits HCT116 cells proliferation with an IC 50 of 6 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 IC 50 values <5 nM.
SCH-1473759 at a low dose of 5 mg/kg (ip, bid) is well-tolerated in a continuous dosing schedule and shows 50% tumor growth inhibition(TGI) on day 16. A higher dose of 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 shows good exposure in all species with the clearance being high in rodents and moderate in dog and monkey. The half-life is also moderate, but the tissue distribution is high. 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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-10483 | 1094067-13-6 SCH-1473759 hydrochloride | 1094067-13-6 | 2mg | 1800元 |
2024/08/19 | HY-10483 | 1094067-13-6 SCH-1473759 hydrochloride | 1094067-13-6 | 5mg | 2800元 |