Nutlin-3b
Based on 2 publication(s) in Google Scholar
Nutlin-3b, the inactive form of Nutlin-3 (HY-50696), is a p53/MDM2 inhibitor with an IC50 of 13.6 μM. Nutlin-3b is 150 times less potent in binding to MDM2 than Nutlin-3a (HY-10029). Nutlin-3b is promising for research of cancers.
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- Pureté: 98.63%
- CAS No.: 675576-97-3
- Formule: C30H30Cl2N4O4
- Masse moléculaire:581.49
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Nutlin-3b
More
Activité biologique
IC50: 13.6 μM (MDM2/p53)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
10 μM
Compound: Nutlin-3
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
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[PMID: 28797774] |
| A549 | IC50 |
2.4 μM
Compound: Nutlin-3
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Antiproliferative activity against human A549 cells measured after 24 hrs by CCK8 assay
Antiproliferative activity against human A549 cells measured after 24 hrs by CCK8 assay
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[PMID: 31047751] |
| HCT-116 | GI50 |
1.52 μM
Compound: Nutlin-3
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Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 3 days by SRB assay
Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 3 days by SRB assay
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[PMID: 28743509] |
| HCT-116 | IC50 |
11.3 μM
Compound: Nutlin-3
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Antiproliferative activity against human HCT-116 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
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[PMID: 36989812] |
| HCT-116 | IC50 |
28.4 μM
Compound: Nutlin-3
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Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
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[PMID: 28797774] |
| HCT-116 | IC50 |
4 μM
Compound: Nutlin-3
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Antiproliferative activity against human HCT116 cells measured after 24 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells measured after 24 hrs by CCK8 assay
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[PMID: 31047751] |
| MCF7 | IC50 |
12.1 μM
Compound: Nutlin-3
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Antiproliferative activity against human MCF7 cells measured after 24 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells measured after 24 hrs by CCK8 assay
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[PMID: 31047751] |
| MCF7 | IC50 |
14.9 μM
Compound: Nutlin-3
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
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[PMID: 28797774] |
| SAOS-2 | IC50 |
20.16 μM
Compound: Nutlin-3
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Cytotoxicity against p53 deficient human Saos2 cells assessed as cell growth inhibition after 24 hrs by MTT assay
Cytotoxicity against p53 deficient human Saos2 cells assessed as cell growth inhibition after 24 hrs by MTT assay
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[PMID: 28482147] |
| U2OS | IC50 |
2.66 μM
Compound: Nutlin-3
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Cytotoxicity against wild type p53 expressing human U2OS cells assessed as cell growth inhibition after 24 hrs by MTT assay
Cytotoxicity against wild type p53 expressing human U2OS cells assessed as cell growth inhibition after 24 hrs by MTT assay
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[PMID: 28482147] |
| U-87MG ATCC | IC50 |
5.93 μM
Compound: Nutlin-3
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Cytotoxicity against human U87 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 24 hrs by MTT assay
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[PMID: 28916339] |
Nutlin-3b (0-8 μM, 8 h) shows a potent antiproliferative activity in MDA-MB-435 and SW480 cells harboring mutant p53[1].
Nutlin-3b (10 μM, 24 h and 48 h) has no influence on cell proliferation and apoptosis in wild-type p53 (HCT116)[1].
Nutlin-3b (10 μM, 4, 24 and 48 h) slightly decreases p53 mRNA levels in sensitive liposarcoma cells[2].
Nutlin-3b (20 μM, 60 min) interfere with P-gp-mediated drug efflux in UKF-NB-3rVCR10 neuroblastoma cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 675576-97-3
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Appearance Solid
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Masse moléculaire 581.49
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Formule C30H30Cl2N4O4
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Color Off-white to yellow
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SMILES
O=C1NCCN(C(N2[C@@H](C3=CC=C(Cl)C=C3)[C@@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(OC)C=C5OC(C)C)=O)C1
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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 (2)
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Journal Impact Factor
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Most Recent
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bioRxiv
2024 Nov 4:2024.10.08.617155. PMID: 39415993
Solvant et solubilité
DMSO : ≥ 100 mg/mL (171.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (4.30 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.
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Vassilev LT, et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 2004 Feb 6;303(5659):844-8. [Content Brief]
[2]. Müller CR, et al. Potential for treatment of liposarcomas with the MDM2 antagonist Nutlin-3A. Int J Cancer. 2007 Jul 1;121(1):199-205. [Content Brief]
[3]. Michaelis M, et al. Reversal of P-glycoprotein-mediated multidrug resistance by the murine double minute 2 antagonist nutlin-3. Cancer Res. 2009 Jan 15;69(2):416-21. [Content Brief]
[4]. Zhang F, et al. MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport. Biochem Pharmacol. 2011 Jul 1;82(1):24-34. [Content Brief]
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 | 1.7197 mL | 8.5986 mL | 17.1972 mL | 42.9930 mL |
| 5 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL | 8.5986 mL | |
| 10 mM | 0.1720 mL | 0.8599 mL | 1.7197 mL | 4.2993 mL | |
| 15 mM | 0.1146 mL | 0.5732 mL | 1.1465 mL | 2.8662 mL | |
| 20 mM | 0.0860 mL | 0.4299 mL | 0.8599 mL | 2.1497 mL | |
| 25 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7197 mL | |
| 30 mM | 0.0573 mL | 0.2866 mL | 0.5732 mL | 1.4331 mL | |
| 40 mM | 0.0430 mL | 0.2150 mL | 0.4299 mL | 1.0748 mL | |
| 50 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8599 mL | |
| 60 mM | 0.0287 mL | 0.1433 mL | 0.2866 mL | 0.7166 mL | |
| 80 mM | 0.0215 mL | 0.1075 mL | 0.2150 mL | 0.5374 mL | |
| 100 mM | 0.0172 mL | 0.0860 mL | 0.1720 mL | 0.4299 mL |
Nutlin-3b Related Classifications
HY-15335 Related Classifications
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