NVP-CGM097

For research use only.

Catalog No.S7875 Synonyms: CGM-097, CGM 097, CGM 097, NVP CGM097

3 publications

NVP-CGM097 Chemical Structure

Molecular Weight(MW): 659.26

NVP-CGM097 is a highly potent and selective MDM2 inhibitor with Ki value of 1.3 nM for hMDM2 in TR-FRET assay. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.

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Selleck's NVP-CGM097 has been cited by 3 publications

1 Customer Review

  • (C) SACi2 effects are dependent on MT-kinetochore attachments. The graph shows percentage of cells undergoing forced mitotic exit by SACi2 or DMSO in various pretreatment conditions (mean ± SEM, three independent assays). Nocodazole (Noc) was used at 70 nM and 3 μM, vinblastine (Vbl) at 1 μM, taxol (Tx) at 600 nM and monastrol (Mon) at 100 μM concentrations and were added 8 h before addition of DMSO or SACi2. MG132 (20 μM) was added 1 h before nocodazole.

    Carcinogenesis, 2013, 34(2):436-445.. NVP-CGM097 purchased from Selleck.

Purity & Quality Control

Choose Selective Mdm2 Inhibitors

Biological Activity

Description NVP-CGM097 is a highly potent and selective MDM2 inhibitor with Ki value of 1.3 nM for hMDM2 in TR-FRET assay. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.
Targets
hMDM2 [1]
(Cell-free assay)
1.7 nM
In vitro

NVP-CGM097 binding to MDM2 is species dependent. It was shown to be selective for the p53:MDM2 interaction compared to the p53:MDM4 interaction (1176-fold selectivity) and the Ras:Raf interaction (3000-fold selectivity). In addition, NVP-CGM097 showed no significant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein-protein interactions. NVP-CGM097 was able to significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM, demonstrating its ability to inhibit the p53:MDM2 interaction in living cells. NVP-CGM097 treatment leads to p53 nuclear translocation that results in cell growth inhibition in a p53-dependent manner[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SJSA1 cells MnnJSpVv[3Srb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxZjDoeY1idiCVSmPBNUBk\WyuczygS2k2OD1yLkO1JO69VQ>? NIr4cZozPjF6MUi1NS=>
HCT116 cells NWn2VpFUTnWwY4Tpc44h[XO|YYm= MkK2TY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib3[gbJVu[W5iSFPUNVE3KGOnbHzzJIV5eHKnc4PpcocheDV|LDDJR|UxRTBwNEW0JO69VQ>? MXWyOlE5OTh3MR?=
PC3 cells M2X2NWZ2dmO2aX;uJIF{e2G7 NU\hTXltUW6qaXLpeIlwdiCxZjDtWG9TSzJiaX6gbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQVvUJJBpd3OyaH;yfYxifGmxbjDheEBUPDd|IHHmeIVzKDFiaIKsJGlEPTB;MD6wNlIh|ryP M2Ox[FI3OTB{NUC2

... Click to View More Cell Line Experimental Data

In vivo After iv administration, the total blood clearance (CL) of NVP-CGM097 was 5 mL/min/kg for mouse, 7 mL/min/kg for rat, 3 mL/min/kg for dog, and 4 mL/min/kg for monkey. On the basis of the respective hepatic blood flows, NVP-CGM097 showed a consistent low total blood CL in all species (5-10% of hepatic blood flow). The apparent terminal half-life (t1/2) was long in rodents and monkey (6-12 h) but was comparatively longer in dogs (20 h). After oral dosing, the compound was well absorbed with Tmax occurring between 1 and 4.5 h in all species tested. The oral bioavailability (%F) was high in mouse, rat, and dog and moderate in monkey. NVP-CGM097 was able to inhibit the interaction between p53 and MDM2 and reactivate the p53 pathway in vivo in a MDM2-amplified SJSA-1 human tumor model. p21 mRNA levels were found to increase concomitantly with levels of compound 1 in tumor-bearing rats dosed at 30 mg/kg. Daily treatment with NVP-CGM097 dose dependently and significantly inhibited SJSA-1 tumor growth in rats[1].

Protocol

Cell Research:[2]
- Collapse
  • Cell lines: Bon1 cells, NCI-H727 cells, Got1 cells
  • Concentrations: 0.1 nM-2500 nM
  • Incubation Time: 48 hrs, 96 hrs, 144 hrs or 216 hrs
  • Method: Cells were seeded in appropriate densities (Bon1 cells: 1500 cells/well, NCI-H727 cells: 2000 cells/well, Got1 cells: 50000 cells/well) into 96-well plates and grown for 24 hrs in complete medium containing serum/antibiotic. The next day, the cells were incubated with various concentrations of NVP-CGM097 (0.1 nM-2500 nM), 5-fluorouracil (100 nM-100 µM), streptozotocin (1 nM-100 µM), temozolomide (1 µM-1 mM), everolimus (10 nM) or octreotide (100 nM-10 µM) in 10 % FBS medium (antibiotic-free). After 48 hrs, 96 hrs, 144 hrs or 216 hrs the metabolic activity was measured with "Cell Titer 96 Aqueous One Solution" cell proliferation assay. The measurement was performed at 492 nm with an ELISA plate reader.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Sprague-Dawley rat
  • Dosages: 1 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 65 mg/mL (98.59 mM)
Ethanol 65 mg/mL (98.59 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 659.26
Formula

C38H47ClN4O4

CAS No. 1313363-54-0
Storage powder
in solvent
Synonyms CGM-097, CGM 097, CGM 097, NVP CGM097
Smiles COC1=CC2=C(C=C1OC(C)C)C(N(C(=O)C2)C3=CC=C(C=C3)N(C)CC4CCC(CC4)N5CCN(C)C(=O)C5)C6=CC=C(Cl)C=C6

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID