An inhibitor of the MDM2-p53 interaction
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Product Type

Biochemicals

Research Area

Cancer
Transcription Factors

NVP-CGM097

Item No. 29519

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S)-1-(4-chlorophenyl)-1,4-dihydro-6-methoxy-7-(1-methylethoxy)-2-[4-[methyl[[trans-4-(4-methyl-3-oxo-1-piperazinyl)cyclohexyl]methyl]amino]phenyl]-3(2H)-isoquinolinone
CAS Number
1313363-54-0
Molecular Formula
C38H47ClN4O4
Formula Weight
659.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
267 nm
SMILES
CN1CCN([C@H]2CC[C@H](CN(C)C3=CC=C(N4[C@@H](C5=CC=C(Cl)C=C5)C6=CC(OC(C)C)=C(OC)C=C6CC4=O)C=C3)CC2)CC1=O
InChi Code
InChI=1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26-,31-,38-/m0/s1
InChi Key
CLRSLRWKONPSRQ-IIPSPAQQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $103

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    5 mg

    $354

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    10 mg

    $653

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    Cayman Chemical
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    Product Description

    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 (Ki = 1.3 nM) over dog, mouse, and rat Mdm2 (Kis = 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Weisberg, E., Halilovic, E., Cooke, V.G., et al. Inhibition of wild-type p53-expressing AML by the novel small molecule HDM2 inhibitor CGM097. Mol. 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 tumors. J. Med. Chem. 58(16), 6348-6358 (2015).