CD532

SKU: orb1689922

Description

CD532 is a potent and selective Aurora A kinase inhibitor (IC50 = 45 nM) that induces a conformational change in the kinase, leading to MYCN degradation. It is a valuable chemical probe for studying cancers, particularly neuroblastoma, in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Epigenetics & Chromatin, Immunology & Inflammation

Key Properties

• CAS Number: 1639009-81-6
• MW: 522.52
• Purity: 99.49% (May vary between batches)
• Formula: C₂₆H₂₅F₃N₈O
• SMILES: N(C=1C=C(NN1)C2CCCC2)C3=NC(NC4=CC=C(NC(NC5=CC(C(F)(F)F)=CC=C5)=O)C=C4)=NC=C3
• Target: Aurora Kinase
• Solubility: DMSO:200 mg/mL (382.76 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.57 mM)

Bioactivity

• Target IC50:
  Aurora A:45 nM|Kelly:146.7 nM(EC50）|SK-N-BE cells:223.2 nM(EC50）
• In Vivo:
  In mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma, CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival. In MYCN-amplified neuroblastoma xenografts, CD532 (60 mg/kg; i.p. for 2 days) reduces the level of MYCN protein. CD532 (20 mg/kg; i.p.) in mice exhibits a serum half-life of ~1.5 hours and an AUC0-24 of 27 μM•h.
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• In Vitro:
  In MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, CD532 (1-10000 nM; 72 h) exhibits cytotoxicity with EC50s of 223.2 nM and 146.7 nM, respectively. In SK-N-BE(2) cells, CD532 (0.1-1 μM; 24 h) causes a dose-dependent loss of MYCN protein. Furthermore, CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AuroraKinase, Aurora Kinase, Aurora A, 1 [4 ({4 [(5 cyclopentyl 1H pyrazol 3 yl)imino] 1,4 dihydropyrimidin 2 yl}amino)phenyl] 3 [3 (trifluoromethyl)phenyl]urea, 1[4({4[(5cyclopentyl1Hpyrazol3yl)imino]1,4dihydropyrimidin2yl}amino)phenyl]3[3(trifluoromethyl)phenyl]urea, CD 532, CD532, CD-532

Compound Identifiers

PubChem CID

77232197