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(SCH1473759; SCH 1473759)
SCH-1473759 Chemical Structure
|Product name: SCH-1473759|
|Cat. No.: HY-10482|
SCH 1473759 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).
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 .
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.
Clinical trial: N/A
|M.Wt||426.54||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.3444 mL||11.7222 mL||23.4445 mL|
|5 mM||0.4689 mL||2.3444 mL||4.6889 mL|
|10 mM||0.2344 mL||1.1722 mL||2.3444 mL|
. Basso AD, Liu M, Gray K, 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.
CAS No.: 1094067-13-6 In-stock
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