NVP-CGM097
Based on 4 publication(s) in Google Scholar
NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
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- Pureté: 99.80%
- CAS No.: 1313363-54-0
- Formule: C38H47ClN4O4
- Masse moléculaire:659.26
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NVP-CGM097
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Activité biologique
Description
IC50 & Target
IC50: 1.7±0.1 nM (hMDM2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
15983 nM
Compound: 1, NVP-CGM097
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Inhibition of cell proliferation of human HCT116 cells deficient with p53 gene
Inhibition of cell proliferation of human HCT116 cells deficient with p53 gene
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[PMID: 26181851] |
| HCT-116 | IC50 |
454 nM
Compound: 1, NVP-CGM097
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Inhibition of cell proliferation of human HCT116 cells expressing p53
Inhibition of cell proliferation of human HCT116 cells expressing p53
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[PMID: 26181851] |
| SAOS-2 | IC50 |
20464 nM
Compound: 1, NVP-CGM097
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Inhibition of cell proliferation of human Saos2 cells deficient with p53 gene
Inhibition of cell proliferation of human Saos2 cells deficient with p53 gene
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[PMID: 26181851] |
| SJSA-1 | GI50 |
0.35 μM
Compound: 1, NVP-CGM097
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Inhibition of cell proliferation of human SJSA1 cells
Inhibition of cell proliferation of human SJSA1 cells
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[PMID: 26181851] |
| SJSA-1 | IC50 |
353 nM
Compound: 1, NVP-CGM097
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Inhibition of cell proliferation of human SJSA1 cells expressing p53
Inhibition of cell proliferation of human SJSA1 cells expressing p53
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[PMID: 26181851] |
In Vitro
NVP-CGM097 binds to human MDM2 with an IC50 of 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). In addition, NVP-CGM097 shows 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 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, demonstrating its ability to inhibit the p53:MDM2 interaction in living cells. In addition, NVP-CGM097 activity against the p53:MDM2 interaction is assessed in proliferation assays using either wild-type p53 or p53 null cells. 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 inhibtis HCT116 (p53WT/WT) with IC50 of 454±136 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1313363-54-0
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Appearance Solid
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Masse moléculaire 659.26
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Formule C38H47ClN4O4
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Color Off-white to yellow
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SMILES
ClC(C=C1)=CC=C1[C@@H](C2=CC(OC(C)C)=C(OC)C=C2C3)N(C4=CC=C(N(C[C@@H]5CC[C@@H](N6CC(N(C)CC6)=O)CC5)C)C=C4)C3=O
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Synonyms
CGM097
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cells
MDM2 Drives Proteasome Inhibitor Resistance and Represents a TP53-Independent Therapeutic Vulnerability in Multiple Myeloma. [Abstract]2026 May 1;15(9):831. PMID: 42121932 -
Cells
PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]2026 Mar 5;15(5):473. PMID: 41827906 -
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Biomed Pharmacother
An anti-GD2 aptamer-based bifunctional spherical nucleic acid nanoplatform for synergistic therapy targeting MDM2 for retinoblastoma. [Abstract]2024 May:174:116437. PMID: 38522240
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (151.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.79 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Cell Assay[1]
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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
Rats[1]
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 po 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5169 mL | 7.5843 mL | 15.1685 mL | 37.9213 mL |
| 5 mM | 0.3034 mL | 1.5169 mL | 3.0337 mL | 7.5843 mL | |
| 10 mM | 0.1517 mL | 0.7584 mL | 1.5169 mL | 3.7921 mL | |
| 15 mM | 0.1011 mL | 0.5056 mL | 1.0112 mL | 2.5281 mL | |
| 20 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8961 mL | |
| 25 mM | 0.0607 mL | 0.3034 mL | 0.6067 mL | 1.5169 mL | |
| 30 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2640 mL | |
| 40 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9480 mL | |
| 50 mM | 0.0303 mL | 0.1517 mL | 0.3034 mL | 0.7584 mL | |
| 60 mM | 0.0253 mL | 0.1264 mL | 0.2528 mL | 0.6320 mL | |
| 80 mM | 0.0190 mL | 0.0948 mL | 0.1896 mL | 0.4740 mL | |
| 100 mM | 0.0152 mL | 0.0758 mL | 0.1517 mL | 0.3792 mL |
NVP-CGM097 Related Classifications
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