A dual modulator of p53-MDM2 interaction and NF-κB signaling
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CAY10681

Item No. 15573

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
1542066-69-2
Molecular Formula
C30H26BrN5O
Formula Weight
552.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
231, 252 nm
SMILES
O=C1N(CCCN2C=CN=C2)C(C3=CC=C(Br)C=C3)C4=C1N(CC5=CC=CC=C5)N=C4C6=CC=CC=C6
InChi Code
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
InChi Key
HZXBRCFEDOCBBP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $81

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    5 mg

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    10 mg

    $593

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    25 mg

    $1,084

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    Cayman Chemical
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    Product Description

    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.1 It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53.1 CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65.1 It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 µM).1 CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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).