An inhibitor of MDM2-p53 interaction
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Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

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Product Type

RO8994

Item No. 25674

Technical Information
Formal Name
(2'S,3R,4'S,5'R)-N-[4-(aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide
CAS Number
1309684-94-3
Molecular Formula
C31H31Cl2FN4O4
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 12.5 mg/mlDMSO: 14 mg/mlEthanol: 5 mg/ml
λmax
212, 270, 300 nm
SMILES
O=C(NC1=C(OC)C=C(C(N)=O)C=C1)[C@H](N[C@H]2CC(C)(C)C)[C@H](C3=CC=CC(Cl)=C3F)[C@]2(C4=CC=C(Cl)C=C4N5)C5=O
InChi Code
InChI=1S/C31H31Cl2FN4O4/c1-30(2,3)14-23-31(18-10-9-16(32)13-21(18)37-29(31)41)24(17-6-5-7-19(33)25(17)34)26(38-23)28(40)36-20-11-8-15(27(35)39)12-22(20)42-4/h5-13,23-24,26,38H,14H2,1-4H3,(H2,35,39)(H,36,40)(H,37,41)/t23-,24-,26+,31+/m0/s1
InChi Key
MURAVORBGFDSMA-ISKXDESKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).1 It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, Z., Ding, Q., Liu, J.J., et alDiscovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg. Med. Chem. 22(15), 4001-4009 (2014).