1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

SCH-1473759 (Synonyms: SCH1473759; SCH 1473759)

Cat. No.: HY-10482
Handling Instructions

SCH 1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.

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SCH-1473759 Chemical Structure

SCH-1473759 Chemical Structure

CAS No. : 1094069-99-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $206 In-stock
2 mg $120 In-stock
5 mg $220 In-stock
10 mg $320 In-stock
50 mg $750 Backordered
100 mg $1150 Backordered
200 mg   Get quote  
500 mg   Get quote  

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Description

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)[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]. Protocol(Only for Reference) [1] Kinase assay: Aurora A and Aurora B kinase assays were performed in low protein binding 384-well plates. Compounds were diluted in 100% DMSO to the desired concentrations. For the Aurora A assay, each reaction consisted of 8 nM enzyme (Aurora A, Upstate), 100 nM Tamra-PKAtide (Molecular Devices, 5TAMRA-GRTGRRNSICOOH ), 25 uM ATP, 1 mM DTT, and kinase buffer (10 mM Tris, 10 mM MgCl2, 0.01% Tween 20). For the Aurora B assay, each reaction consisted of 26 nM enzyme (Aurora B, Invitrogen), 100 nM Tamra-PKAtide (Molecular Devices, 5TAMRA-GRTGRRNSICOOH ), 50 uM ATP, 1 mM DTT, and kinase buffer (10 mM Tris, 10 mM MgCl2, 0.01% Tween 20). Dose-response curves were plotted from inhibition data generated in duplicate, from 8 point serial dilutions of inhibitory compounds. Concentration of compound was plotted against kinase activity, calculated by degree of fluorescent polarization. To generate IC50 values, the dose-response curves were then fitted to a standard sigmoidal curve and IC50 values were derived by nonlinear regression analysis. Other kinases were tested in-house or by utilizing Millipore Kinase Profiling service to generate selectivity data for SCH 1473759 (12k). Assays were run at ATP concentrations close to the Km of the respective enzyme being tested. Cell Cycle Analysis: HCT-116 cells were plated using 1x106 cells per 10 cm tissue culture dish. The next day cells were treated with compound (0.1% final DMSO concentration) and 24 hours later collected and centrifuged for 1 minute at 1,000 rpm. Cell pellet was resuspended in 0.5 ml PBS and the solution was transferred to cold 70% methanol and incubated at -20°C for 30 minutes. Cells were then centrifuged for one minute at 1,000 rpm, the supernatant was removed, pellet washed with 2 ml PBS, centrifuged, and supernatant removed. Cells were resuspended in 0.5 ml propidium iodine stain (0.1 mM EDTA, 0.05 mg/ml RNase, 50 ug/ml propidium iodine), transferred to a filter cap tube and read by fluorescence activated cell sorting (FACS).

Preparing Stock Solutions
Concentration Volume (DMSO) Mass 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
M.Wt

426.54

Formula

C₂₀H₂₆N₈OS

CAS No.

1094069-99-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

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SCH-1473759
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