NVP-CGM097 sulfate

An inhibitor of the MDM2-p53 interaction

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2mg

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1040.00

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5mg

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50mg

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11970.00

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100mg

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200mg

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500mg

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Background

NVP-CGM097 is an inhibitor of the protein-protein interaction between murine double minute 2 (MDM2) and p53 (IC₅₀ = 1.7 nM for human MDM2 in a TR-FRET assay).¹ It is selective for human MDM2 (K_i = 1.3 nM) over dog, mouse, and rat Mdm2 (K_is = 20.5, 65.9, and 47.4 nM, respectively).² NVP-CGM097 selectively inhibits proliferation of acute myeloid leukemia (AML) cells expressing wild-type p53 (IC₅₀s = 50-1,000 nM) over AML cells expressing mutant p53 (IC₅₀s = >1,000 nM).¹ It induces tumor regression in a patient-derived xenograft (PDX) mouse model of AML when administered at a dose of 100 mg/kg per day.¹

1.Weisberg, E., Halilovic, E., Cooke, V.G., et al.Inhibition of wild-type p53-expressing AML by the novel small molecule HDM2 inhibitor CGM097Mol. Cancer Ther.14(10)2249-2259(2015) 2.Holzer, P., Masuya, K., Furet, P., et al.Discovery of a dihydroisoquinolinone derivative (NVP-CGM097): A highly potent and selective MDM2 inhibitor undergoing phase 1 clinical trials in p53wt tumorsJ. Med. Chem.58(16)6348-6358(2015)