Home Tools
Log in
Cart

NVP-CGM097

Catalog No. TQ0231   CAS 1313363-54-0
Synonyms: CGM097

NVP-CGM097 (CGM097) is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
NVP-CGM097 Chemical Structure
NVP-CGM097, CAS 1313363-54-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 79.00
2 mg In stock $ 117.00
5 mg In stock $ 217.00
10 mg In stock $ 359.00
25 mg In stock $ 593.00
50 mg In stock $ 863.00
100 mg In stock $ 1,190.00
1 mL * 10 mM (in DMSO) In stock $ 316.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 98.92%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description NVP-CGM097 (CGM097) is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
Targets&IC50 MDM2:1.7 nM
In vitro NVP-CGM097 binds to human MDM2(IC50: 1.7 nM) and shows high selectivity over MDM4 (IC50: 2000 nM). NVP-CGM097 is about four times more potent than Nutlin-3a (IC50: 8 nM). NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 is able to significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 inhibits HCT116 (p53WT/WT, IC50: 454±136 nM).
In vivo p21 mRNA levels are found to increase concomitantly with levels of NVP-CGM097 in tumor-bearing rats dosed at 30 mg/kg. The PD response is biphasic and prolonged up to 24 h. Additional p53 target genes such as MDM2 and PUMA mRNA levels are assessed in the tumor samples as well and showed similar behavior. Daily treatment with NVP-CGM097 dose-dependently and significantly inhibits SJSA-1 tumor growth in rats. It promotes stable disease at 20 mg/kg, which is associated with a plasma AUC0-24 of 163 μM?h. After iv administration, the total blood clearance (CL) of NVP-CGM097 is 5 mL/min per kg for mouse, 7 mL/min per kg for rat, 3 mL/min per kg for dog, and 4 mL/min per kg for monkey. The apparent terminal half-life (t1/2) is long in rodents and monkey (6-12 h) but is comparatively longer in dogs (20 h). After oral dosing, NVP-CGM097 is well absorbed with Tmax occurring between 1 and 4.5 h in all species tested.
Cell Research Two pairs of cell lines are used to assess NVP-CGM097 p53-dependent antiproliferative effects: (1) an isogenic pair of HCT116 cell lines either expressing wild-type p53 or knocked-out for the p53 gene and (2) a nonisogenic pair of osteosarcoma cell lines either endogenously expressing wild-type p53 and amplified for MDM2 (SJSA-1 cells) or null for p53 (SAOS-2 cells).
Animal Research Female athymic rats bearing subcutaneous xenotransplants of SJSA-1 tumors (n=5-12) are treated at 5, 10, 20, or 30 mg/kg or three times a week on Monday, Wednesday, and Friday (3qw M, W, F) at 30 or 70 mg/kg p.o for 14 days. Plasma AUCs are determined at the end of the study. Positive numbers indicate the percentage of tumor growth inhibition (T/C); negative numbers indicate the percentage of tumor regression.
Synonyms CGM097
Molecular Weight 659.26
Formula C38H47ClN4O4
CAS No. 1313363-54-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48 mg/mL (72.81 mM )

H2O: Insoluble

TargetMolReferences and Literature

1. Holzer 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. 2015 Aug 27;58(16):6348-58

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library HIF-1 Signaling Pathway Compound Library Anti-Cancer Metabolism Compound Library Pyroptosis Compound Library Endoplasmic Reticulum Stress Compound Library Apoptosis Compound Library Clinical Compound Library

Related Products

Related compounds with same targets
Cbl-b-IN-6 YH239-EE Heclin Cbl-b-IN-8 Nutlin-3b Cbl-b-IN-7 SMIP004 SCFSkp2-IN-2

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

NVP-CGM097 1313363-54-0 Apoptosis Ubiquitination E1/E2/E3 Enzyme Mdm2 Ubiquitin ligase inhibit MDM-2/p53 CGM-097 E3 ligating enzyme CGM 097 Ubiquitin activating enzyme NVP CGM097 Inhibitor CGM097 E2 conjugating enzyme NVPCGM097 E1 activating enzyme NVP-CGM-097 Ubiquitin conjugating enzyme NVP-CGM 097 inhibitor

 

TargetMol