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SCH-1473759 hydrochloride

Name: SCH-1473759 hydrochloride
Brand: TargetMol
SKU: T12864
Rating: 4.5 (1 reviews)

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Catalog No. T12864Cas No. 1094067-13-6

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

SCH-1473759 hydrochloride

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Purity: 98.29%

Catalog No. T12864Cas No. 1094067-13-6

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

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$380	5 days	5 days
5 mg	Inquiry	5 days	5 days
10 mg	Inquiry	5 days	5 days
1 mL x 10 mM (in DMSO)	Inquiry	5 days	5 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:98.29%

Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	SCH-1473759 hydrochloride is an inhibitor of aurora(aurora A and B with IC50s of 4 and 13 nM, respectively).
Targets&IC50	Aurora A:4 nM, Aurora B:13 nM
In vitro	SCH-1473759 directly binds to aurora A and B (Kds of 20 and 30 nM, respectively) and inhibits the Src family of kinases (IC50 less than 10 nM), Chk1 (IC50 of 13 nM), VEGFR2 (IC50 of 1 nM), and IRAK4 (IC50 of 37 nM). It inhibits tumor cell lines from various tissues, including breast, ovarian, prostate, lung, colon, brain, gastric, renal, skin, and leukemia. The most sensitive cell lines include A2780, LNCap, N87, Molt4, K562, and CCRF-CEM with IC50 values <5 nM [2].
In vivo	SCH-1473759(5 mg/kg ,ip, bid) was well tolerated in the continuous dosing regimen and showed 50% tumor growth inhibition (TGI) on day 16. SCH-1473759(10mg/kg,ip, bid) is well-tolerated in an intermittent schedule (5 days on, 5 days off) and gave 69% TGI on day 16. SCH-1473759 showed good exposure in all species, with high clearance rates in rodents and moderate clearance rates in dogs and monkeys.The half-life is also moderate, but the tissue distribution is high[1]. SCH 1473759 dose- and schedule-dependent anti-tumor activity in four human tumor xenograft models. Further, the efficacy is enhanced in combination with taxanes and found to be most efficacious when SCH 1473759 is dosed 12-h post-taxane treatment[2].

Chemical Properties

Molecular Weight	463
Formula	C₂₀H₂₇ClN₈OS
Cas No.	1094067-13-6
Smiles	Cl.CCN(Cc1cc(Nc2nc(C)cn3c(cnc23)-c2cn[nH]c2)sn1)C(C)(C)CO
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 70 mg/mL (151.19 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.16 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1598 mL	10.7991 mL	21.5983 mL	107.9914 mL
5 mM	0.4320 mL	2.1598 mL	4.3197 mL	21.5983 mL
10 mM	0.2160 mL	1.0799 mL	2.1598 mL	10.7991 mL
20 mM	0.1080 mL	0.5400 mL	1.0799 mL	5.3996 mL
50 mM	0.0432 mL	0.2160 mL	0.4320 mL	2.1598 mL
100 mM	0.0216 mL	0.1080 mL	0.2160 mL	1.0799 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc