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CD532 is A potent inhibitor of Aurora A kinase with an IC50 of 45 nM. It breaks the natural conformation of Arora-A, drives N-Myc degradation in n-myC-driven cancers, and also exhibits anti-proliferative effects.
Brand: BCM
In Vitro: CD532 (1-10000 nM; 72 h) shows cytotoxic in MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, with EC 50 s of 223.2 nM and 146.7 nM, respectively. CD532 (0.1-1 μM; 24 h) causes dose-dependent loss of MYCN protein in SK-N-BE(2) cells. CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells. Cell Viability Assay 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 EC 50 s of 223.2 nM and 146.7 nM, respectively. Cell Cycle Analysis 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 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.
pKa: 13.86±0.70(Predicted)
Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.
Isomeric SMILES: C1CCC(C1)C2=CC(=NN2)NC3=NC(=NC=C3)NC4=CC=C(C=C4)NC(=O)NC5=CC=CC(=C5)C(F)(F)F
InChIKey: GBMIFBVLJSCVJT-UHFFFAOYSA-N
InChI: InChI=1S/C26H25F3N8O/c27-26(28,29)17-6-3-7-20(14-17)33-25(38)32-19-10-8-18(9-11-19)31-24-30-13-12-22(35-24)34-23-15-21(36-37-23)16-4-1-2-5-16/h3,6-16H,1-2,4-5H2,(H2,32,33,38)(H3,30,31,34,35,36,37)
Attribute [Chem Name] 1-[4-[[4-[(5-cyclopentyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]phenyl]-3-[3-(trifluoromethyl)phenyl]urea [Synonym] CD532 [CAS No.] 1639009-81-6 [Formula] C26H25F3N8O [Molecular] 522.52 [Form] Solid Powder [Storage] Sealed in dry. Stored at -20°C.
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