计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
SCH-1473759 hydrochloride is an aurora inhibitor with IC 50 s of 4 and 13 nM for aurora A and B, respectively.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Mice: Anti-tumor efficacy of SCH 1473759 dosed i.p. is evaluated in mice bearing established A2780 ovarian tumor xenografts. Three schedules are tested at their respective maximum tolerated doses: 10 mg/kg bid (twice daily), 20 mg/kg qd (daily), and 100 mg/kg day 0, 4, 7. Additionally, 60 mg/kg day 0, 4, 7 is tested . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Aurora A 4 nM (IC 50 ) Aurora B 13 nM (IC 50 )
规格
别名
SCH-1473759 盐酸盐
规格或纯度
10mM in DMSO
英文名称
SCH-1473759 hydrochloride
生化机理
SCH-1473759 盐酸盐是一种极光抑制剂，对极光 A 和极光 B 的 IC 50 s 分别为 4 和 13 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO.Cl
PubChem CID
分子量
463.00
技术文档
高级数据
关联靶点（人）
IRAK4
Tchem
白细胞介素-1受体相关激酶4(Interleukin-1 receptor-associated kinase 4)
(1 活性数据)
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(1 活性数据)
AURKB
Tchem
极光激酶B(Aurora kinase B)
(1 活性数据)
CHEK1
Tchem
丝氨酸/苏氨酸蛋白激酶 Chk1(Serine/threonine-protein kinase Chk1)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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