| Identification | Back Directory | [Name]
CAY10682 | [CAS]
1542066-74-9 | [Synonyms]
CAY10682
CAY10682,CAY-10682
4-(4-bromophenyl)-1-[(4-fluorophenyl)methyl]-5-(3-imidazol-1-ylpropyl)-3-phenyl-4H-pyrrolo[3,4-c]pyrazol-6-one
Pyrrolo[3,4-c]pyrazol-6(1H)-one, 4-(4-bromophenyl)-1-[(4-fluorophenyl)methyl]-4,5-dihydro-5-[3-(1H-imidazol-1-yl)propyl]-3-phenyl- | [Molecular Formula]
C30H25BrFN5O | [MOL File]
1542066-74-9.mol | [Molecular Weight]
570.45 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml; Ethanol: 2 mg/ml | [form ]
A crystalline solid |
| Hazard Information | Back Directory | [Description]
(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.1 CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway.2 It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK? (IC50s = 80.5, 78.2, and 57.1 μM, respectively).2 CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 μM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.2 | [References]
1. Vassilev, L.T., Vu, B.T., Graves, B., et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2 Science 303(5659),844-848(2004).
2. Zhuang, C., Miao, Z., Wu, Y., et al. Double-edged swords as cancer therapeutics: Novel, orally active, small molecules simultaneously inhibit p53-MDM2 interaction and the NF-κB pathway J. Med. Chem. 57(3),567-577(2014). |
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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