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SCH-1473759 hydrochloride CAS: 1094067-13-6

Category: Inhibitors
Product Name: SCH-1473759 hydrochloride
Cat No: I000397
CAS No: 1094067-13-6
Molecular Formula: C20H27ClN8OS
Molecular Weight: 463
Solubility: 10 mM in DMSO
Target: Aurora Kinase
IC50: 4 nM (Aurora A); 13 nM (Aurora B)[1].
CAS 1094067-13-6,SCH-1473759 hydrochloride
  • Description

SCH 1473759 Hcl is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.
IC50 Value: 4 nM (Aurora A); 13 nM (Aurora B)[1].
Target: Aurora Kinase
in vitro: Asynchronous cells required 24-h exposure to SCH 1473759 for maximal induction of >4 N DNA content and inhibition of cell growth. However, following taxane- or KSP inhibitor-induced mitotic arrest, less than 4-h exposure induced >4 N DNA content. This finding correlated with the ability of SCH 1473759 to accelerate exit from mitosis in response to taxane- and KSP inhibitor-induced arrest [2].
in vivo: SCH-1473759 showed efficacy and target engagement in A2780 human tumor xenograft model in mouse, and also acceptable pharmacokinetic dosing in dog, monkey and rodents, on target efficacy, as well as a safety profile in dogs[1].

  • References

[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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