1. Cell Cycle/DNA Damage Epigenetics
  2. Aurora Kinase
  3. SCH-1473759 hydrochloride

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

For research use only. We do not sell to patients.

SCH-1473759 hydrochloride Chemical Structure

SCH-1473759 hydrochloride Chemical Structure

CAS No. : 1094067-13-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 269 In-stock
Solution
10 mM * 1 mL in DMSO USD 269 In-stock
Solid
2 mg USD 144 In-stock
5 mg USD 264 In-stock
10 mg USD 384 In-stock
50 mg USD 900 In-stock
100 mg USD 1380 In-stock
200 mg USD 2376 In-stock
500 mg   Get quote  
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Description

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

IC50 & Target[1]

Aurora A

4 nM (IC50)

Aurora B

13 nM (IC50)

In Vitro

SCH-1473759 directly binds to aurora A and B with Kds of 20 and 30 nM, respectively. SCH-1473759 also inhibits the Src family of kinases (IC50<10 nM), Chk1 (IC50=13 nM), VEGFR2 (IC50=1 nM), and IRAK4 (IC50=37 nM). It does not have significant activity (IC50>1000 nM) against 34 other kinases representing different families of the kinome. SCH-1473759 inhibits HCT116 cells proliferation with an IC50 of 6 nM[1]. SCH 1473759 inhibits tumor cell lines from different tissues (breast, ovarian, prostate, lung, colon, brain, gastric, renal, skin, and leukemia). The most sensitive cell lines includ A2780, LNCap, N87, Molt4, K562, and CCRF-CEM with IC50 values <5 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SCH-1473759 at a low dose of 5 mg/kg (ip, bid) is well-tolerated in a continuous dosing schedule and shows 50% tumor growth inhibition(TGI) on day 16. A higher dose of 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 shows good exposure in all species with the clearance being high in rodents and moderate in dog and monkey. 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

463.00

Formula

C20H27ClN8OS

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

[H]Cl.CC1=CN2C(C(NC3=CC(CN(C(C)(CO)C)CC)=NS3)=N1)=NC=C2C4=CNN=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 8.33 mg/mL (17.99 mM; ultrasonic and warming and heat to 60°C)

DMSO : 7.14 mg/mL (15.42 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1598 mL 10.7991 mL 21.5983 mL
5 mM 0.4320 mL 2.1598 mL 4.3197 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.71 mg/mL (1.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.71 mg/mL (1.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.79%

References
Kinase Assay
[1]

Aurora A and Aurora B kinase assays are performed in low protein binding 384-well plates. SCH-1473759 is diluted in 100% DMSO to the desired concentrations. For the Aurora A assay, each reaction consists of 8 nM enzyme Aurora A, 100 nM Tamra-PKAtide, 25μM ATP, 1 mM DTT, and kinase buffer. For the Aurora B assay, each reaction consisted of 26 nM enzyme Aurora B, 100 nM Tamra-PKAtide, 50 μM ATP, 1 mM DTT, and kinase buffer. Dose-response curves are plotted from inhibition data generated in duplicate, from 8 point serial dilutions of SCH-1473759[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cells are plated at a cell density ranging from 625 to 3,750 cells per well and treated in triplicate wells with SCH-1473759 (0.1% final DMSO concentration). A plate is stained at the start of the study (zero hour) and a second plate is incubated for 72 hour at 37°C and then stained. Cells are fixed with fixation solution plus 1,000 nM Hoechst 33342 dye and incubated for 30 minutes. The fixation solution is removed and cells are ished twice with PBS. Then 15 immunofluorescence images are captured at 10X using automated fluorescent microscope [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Anti-tumor efficacy of SCH 1473759 dosed i.p. is evaluated in mice bearing established A2780 ovarian tumor xenografts. Three schedules are tested at their respective maximum tolerated doses: 10 mg/kg bid (twice daily), 20 mg/kg qd (daily), and 100 mg/kg day 0, 4, 7. Additionally, 60 mg/kg day 0, 4, 7 is tested[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.1598 mL 10.7991 mL 21.5983 mL 53.9957 mL
5 mM 0.4320 mL 2.1598 mL 4.3197 mL 10.7991 mL
10 mM 0.2160 mL 1.0799 mL 2.1598 mL 5.3996 mL
15 mM 0.1440 mL 0.7199 mL 1.4399 mL 3.5997 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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SCH-1473759 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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