1. Cell Cycle/DNA Damage Epigenetics
  2. Aurora Kinase
  3. CD532

CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer.

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

CD532 Chemical Structure

CD532 Chemical Structure

CAS No. : 1639009-81-6

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25 mg USD 290 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer[1][2].

IC50 & Target[1]

Aurora A

45 nM (IC50)

In Vitro

CD532 (1-10000 nM; 72 h) is cytotoxic in MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, with EC50s of 223.2 nM and 146.7 nM, respectively[1].
CD532 (0.1-1 μM; 24 h) causes dose-dependent loss of MYCN protein in SK-N-BE(2) cells[1].
CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells[1].

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

Cell Viability Assay[1]

Cell Line: SK-N-BE(2) and Kelly cells
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 72 hours
Result: Inhibited the cell viability of SK-N-BE(2) and Kelly cells, with EC50s of 223.2 nM and 146.7 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: SK-N-BE(2) cells
Concentration: 1 μM
Incubation Time: 4 hours
Result: Resulted in a rapid and potent loss of S-phase and accumulation in both G0/G1 and G2.

Western Blot Analysis[1]

Cell Line: SK-N-BE(2) cells
Concentration: 0.1, 0.25, 0.5, 1 μM
Incubation Time: 2, 4, 6, 24 hours
Result: Causes dose-dependent and time-dependent loss of MYCN protein.
In Vivo

CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival in mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma[1].
CD532 (60 mg/kg; i.p. for 2 days) decreases the level of MYCN protein in MYCN-amplified neuroblastoma xenografts[1].
CD532 (20 mg/kg; i.p.) shows a serum half-life of ~1.5 hours and AUC0-24 of 27 μM•h in mice[1].

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

Animal Model: Homozygous nu/nu mice with SHH-subtype MYCN-expressing medulloblastoma[1]
Dosage: 25 mg/kg
Administration: I.p. twice weekly for 3 weeks
Result: Decreased the level of MYCN protein and tumor volume and increases survival.
Molecular Weight

522.52

Formula

C26H25F3N8O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C1=CC=CC(NC(NC2=CC=C(NC3=NC=CC(NC4=NNC(C5CCCC5)=C4)=N3)C=C2)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (478.45 mM; Need ultrasonic; 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 1.9138 mL 9.5690 mL 19.1380 mL
5 mM 0.3828 mL 1.9138 mL 3.8276 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

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mg/kg

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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).
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
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. 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 1 mM 1.9138 mL 9.5690 mL 19.1380 mL 47.8451 mL
5 mM 0.3828 mL 1.9138 mL 3.8276 mL 9.5690 mL
10 mM 0.1914 mL 0.9569 mL 1.9138 mL 4.7845 mL
15 mM 0.1276 mL 0.6379 mL 1.2759 mL 3.1897 mL
20 mM 0.0957 mL 0.4785 mL 0.9569 mL 2.3923 mL
25 mM 0.0766 mL 0.3828 mL 0.7655 mL 1.9138 mL
30 mM 0.0638 mL 0.3190 mL 0.6379 mL 1.5948 mL
40 mM 0.0478 mL 0.2392 mL 0.4785 mL 1.1961 mL
50 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9569 mL
60 mM 0.0319 mL 0.1595 mL 0.3190 mL 0.7974 mL
80 mM 0.0239 mL 0.1196 mL 0.2392 mL 0.5981 mL
100 mM 0.0191 mL 0.0957 mL 0.1914 mL 0.4785 mL
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CD532 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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CD532
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