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SCH-1473759Aurora A/B inhibitor

SCH-1473759

Catalog No. A3804
Size Price Stock Qty
5mg $261.00 Ship Within 10-14 Days
10mg $336.00 Ship Within 10-14 Days
50mg $906.00 Please Inquire
200mg $2,057.00 Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

SCH-1473759

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Chemical Properties

Cas No. 1094069-99-4 SDF Download SDF
Synonyms SCH1473759;SCH 1473759
Chemical Name 2-[ethyl-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]amino]-2-methylpropan-1-ol
Canonical SMILES CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO
Formula C20H26N8OS M.Wt 426.54
Solubility Soluble in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

IC50 Value: 4 nM (IC50) for Aurora A, and below or equal to 13 nM (IC50) for Aurora B [1]. SCH 1473759, a novel sub-nanomolar Aurora A/B inhibitor. Aurora kinases are required for orderly progression of cells through mitosis, and inhibition of these kinases by siRNA or small molecule inhibitors results in cell death [2]. 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]. Clinical trial: N/A