CAY10681

For research use only. Not for therapeutic Use.

  • CAT Number: R025776
  • CAS Number: 1542066-69-2
  • Molecular Formula: C30H26BrN5O
  • Molecular Weight: 552.476
  • Purity: ≥95%
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Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (K<sub>i</sub> = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (IC<sub>50</sub>s range from 33 to 37 µM). CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.


Catalog Number R025776
CAS Number 1542066-69-2
Synonyms

4-(4-Bromophenyl)-4,5-dihydro-5-[3-(1H-imidazol-1-yl)propyl]-3-phenyl-1-(phenylmethyl)pyrrolo[3,4-c]pyrazol-6(1H)-one; 5-(3-(1H-Imidazol-1-yl)propyl)-1-benzyl-4-(4-bromophenyl)-3-phenyl-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-one

Molecular Formula C30H26BrN5O
Purity ≥95%
Target NF-κB
Storage -20°C
IUPAC Name 1-benzyl-4-(4-bromophenyl)-5-(3-imidazol-1-ylpropyl)-3-phenyl-4H-pyrrolo[3,4-c]pyrazol-6-one
InChI InChI=1S/C30H26BrN5O/c31-25-14-12-24(13-15-25)28-26-27(23-10-5-2-6-11-23)33-36(20-22-8-3-1-4-9-22)29(26)30(37)35(28)18-7-17-34-19-16-32-21-34/h1-6,8-16,19,21,28H,7,17-18,20H2
InChIKey HZXBRCFEDOCBBP-UHFFFAOYSA-N
SMILES C1=CC=C(C=C1)CN2C3=C(C(N(C3=O)CCCN4C=CN=C4)C5=CC=C(C=C5)Br)C(=N2)C6=CC=CC=C6

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