MYCN is an important driver of some cancers however, due to a lack of small molecule binding surfaces it has not been considered drugable. CD532 disrupts the normal confirmation of Aurora A (IC50 = 48nM), driving the degradation of MYCN protein in MYCN-driven cancers. This degradation has been shown to be cytotoxic in MYCN-amplified neuroblastoma cells and has been demonstrated as effective in vivo.
Systematic Name: 1-(4-((4-((5-cyclopentyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)amino)phenyl)-3-(3-(trifluoromethyl)phenyl)urea
SMILES: O=C(NC1=CC=CC(C(F)(F)F)=C1)NC(C=C2)=CC=C2NC3=NC= CC(NC4=NNC(C5CCCC5)=C4)=N3
Molecular Weight: 522.52
Reference: Gustafson, William Clay, et al. "Drugging MYCN through an Allosteric Transition in Aurora Kinase A." Cancer Cell 26.3 (2014): 414-427.
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Tags: MYCN, Cancer, RGNCY-0012, CD532, Aurora A, Neuroblastoma