SCH-1473759

Aurora A/B inhibitor CAS# 1094069-99-4

SCH-1473759

Catalog No. BCC1934----Order now to get a substantial discount!

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SCH-1473759: 5mg $288 In Stock
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Quality Control of SCH-1473759

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Chemical structure

SCH-1473759

3D structure

Chemical Properties of SCH-1473759

Cas No. 1094069-99-4 SDF Download SDF
PubChem ID 25144732 Appearance Powder
Formula C20H26N8OS M.Wt 426.54
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
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
SMILES CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO
Standard InChIKey RHGZQGXELRMGES-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H26N8OS/c1-5-27(20(3,4)12-29)11-15-6-17(30-26-15)25-18-19-21-9-16(14-7-22-23-8-14)28(19)10-13(2)24-18/h6-10,29H,5,11-12H2,1-4H3,(H,22,23)(H,24,25)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

SCH-1473759 Dilution Calculator

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SCH-1473759 Molarity Calculator

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Preparing Stock Solutions of SCH-1473759

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3444 mL 11.7222 mL 23.4445 mL 46.8889 mL 58.6112 mL
5 mM 0.4689 mL 2.3444 mL 4.6889 mL 9.3778 mL 11.7222 mL
10 mM 0.2344 mL 1.1722 mL 2.3444 mL 4.6889 mL 5.8611 mL
50 mM 0.0469 mL 0.2344 mL 0.4689 mL 0.9378 mL 1.1722 mL
100 mM 0.0234 mL 0.1172 mL 0.2344 mL 0.4689 mL 0.5861 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on SCH-1473759

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

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References on SCH-1473759

SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors.[Pubmed:21298383]

Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33.

PURPOSE: 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. We previously reported the synthesis of SCH 1473759, a novel sub-nanomolar Aurora A/B inhibitor. METHODS: We utilized SCH 1473759 and a panel of tumor cell lines and xenograft models to gain knowledge about optimal dosing schedule and chemotherapeutic combinations for Aurora A/B inhibitors. RESULTS: SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and genetic backgrounds. 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. We tested various dosing schedules in vivo and demonstrated SCH 1473759 dose- and schedule-dependent anti-tumor activity in four human tumor xenograft models. Further, the efficacy was enhanced in combination with taxanes and found to be most efficacious when SCH 1473759 was dosed 12-h post-taxane treatment. CONCLUSIONS: SCH 1473759 demonstrated potent mechanism-based activity, and activity was shown to be enhanced in combination with taxanes and KSP inhibitors. This information may be useful for optimizing the clinical efficacy of Aurora inhibitors.

A simple and rapid UHPLC-MS/MS method for the quantitation of the dual aurora kinase A/B inhibitor SCH-1473759 in murine plasma.[Pubmed:27768921]

J Pharm Biomed Anal. 2017 Jan 5;132:223-226.

The Aurora kinase family facilitates cell division through various processes and is overexpressed in a wide variety of human cancers, leading to aneuploidy. For that reason, these enzymes are currently targets of a rising class of anticancer drugs, with some molecules already in therapeutic use. In this study, a new UHPLC-MS/MS method was developed and validated to quantitate a new pan Aurora kinase inhibitor still in preclinical development, SCH-1473759. This bioanalytical method employed a liquid-liquid extraction from plasma using ethyl acetate before evaporation. Calibration range encompassed 0.5-2500ng/mL. The inter- and intra-day accuracy and precision were assessed over five quality control levels; all within limits required by the FDA guidelines. Assay applicability was demonstrated in a first-in-animals study with oral administration, where the maximum plasma concentration (34ng/mL) occurred at 1h, the half-life (1h) was consistent with a previous IV study, and oral bioavailability was poor (F=0.002).

Description

SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.

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