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

CD532 

Cat. No.: HY-112273
Handling Instructions

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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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].

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (478.45 mM; Need ultrasonic)

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
10 mM 0.1914 mL 0.9569 mL 1.9138 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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CD532
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HY-112273
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