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SCH-1473759

Catalog No. T16862 CAS 1094069-99-4

SCH-1473759 is an inhibitor of the aurora (IC50s: 4 and 13 nM for Aurora A and B, respectively).

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SCH-1473759, CAS 1094069-99-4

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SCH-1473759 is an inhibitor of the aurora (IC50s: 4 and 13 nM for Aurora A and B, respectively).
Targets&IC50	Aurora A:4 nM, Aurora B:13 nM
In vitro	SCH-1473759 inhibits HCT116 cells proliferation (IC50: 6 nM). SCH 1473759 inhibits tumor cell lines from different tissues (breast, ovarian, prostate, lung, colon, brain, gastric, renal, skin, and leukemia). 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). SCH-1473759 directly binds to aurora A and B with Kds of 20 and 30 nM, respectively. It does not have significant activity (IC50>1000 nM) against 34 other kinases representing different families of the kinome. The most sensitive cell lines include A2780, LNCap, N87, Molt4, K562, and CCRF-CEM with IC50 values <5 nM [1][2].
In vivo	SCH-1473759 shows good exposure in all species with the clearance being high in rodents and moderate in dog and monkey. SCH 1473759 dose- and schedule-dependent anti-tumor activity in four human tumor xenograft models. SCH-1473759 at a low dose of 5 mg/kg (i.p., 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(i.p., bid) is well-tolerated in an intermittent schedule (5 days on, 5 days off) and gave 69% TGI on day 16. The half-life is also moderate, but tissue distribution is high [1][2].

Molecular Weight	426.54
Formula	C20H26N8OS
CAS No.	1094069-99-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SCH-1473759 1094069-99-4 Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase SCH1473759 SCH 1473759 Inhibitor inhibitor inhibit

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