貨號	規格	價格	上海	北京	武漢	南京
S81959-2mg	≥99%	￥1800.00 S81959-2mg ￥1800.00 2-3天	0 貨期：2-3天	-	-	-
S81959-5mg	≥99%	￥2800.00 S81959-5mg ￥2800.00 2-3天	0 貨期：2-3天	-	-	-
S81959-10mg	≥99%	￥4000.00 S81959-10mg ￥4000.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

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

靶點：

Aurora A:4 nM (IC50);Aurora B:13 nM (IC50);AuroraKinase

體外研究：

SCH-1473759 directly binds to aurora A and B with Kds of 20 and 30 nM, respectively. SCH-1473759 also inhibits the Src family of kinases (IC50<10 nM), Chk1 (IC50=13 nM), VEGFR2 (IC50=1 nM), and IRAK4 (IC50=37 nM). It does not have significant activity (IC50>1000 nM) against 34 other kinases representing different families of the kinome. SCH-1473759 inhibits HCT116 cells proliferation with an IC50 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 IC50 values <5 nM

體內研究：

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

參考文獻：

1. Yu T, et al. Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core. ACS Med Chem Lett. 2010 Jun 7;1(5):214-8. 2. Basso AD, et al. SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors. Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33.

溶解性：

Soluble in DMSO、H2O

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.16 ml	10.799 ml	21.598 ml
5 mM	0.432 ml	2.16 ml	4.32 ml
10 mM	0.216 ml	1.08 ml	2.16 ml
50 mM	0.043 ml	0.216 ml	0.432 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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SCH-1473759 (hydrochloride)