NVX-207
Based on 1 Customer Validation
NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP.
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- Pureté : 98.0%
- CAS No.: 745020-66-0
- Formule: C36H59NO6
- Masse moléculaire:601.86
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 518A2 | IC50 |
2.87 μM
Compound: 5
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Cytotoxicity against human 518A2 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human 518A2 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| A253 cell line | IC50 |
2.02 μM
Compound: 5
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Cytotoxicity against human A253 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human A253 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| A2780 | IC50 |
3.62 μM
Compound: 5
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Cytotoxicity against human A2780 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human A2780 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| A-431 | IC50 |
2.54 μM
Compound: 5
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Cytotoxicity against human A431 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human A431 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| A549 | IC50 |
2.5 μM
Compound: 14; NVX-207
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Growth inhibition of human A549 cells after 18 hrs
Growth inhibition of human A549 cells after 18 hrs
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[PMID: 28500966] |
| A549 | IC50 |
3.44 μM
Compound: 5
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Cytotoxicity against human A549 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human A549 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| HT-29 | IC50 |
2.45 μM
Compound: 5
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Cytotoxicity against human HT-29 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human HT-29 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| MCF7 | IC50 |
2.76 μM
Compound: 5
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Cytotoxicity against human MCF7 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human MCF7 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
| SW-1736 | IC50 |
3.73 μM
Compound: 5
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Cytotoxicity against human SW1736 cells after 96 hrs by SRB colorimetric assay
Cytotoxicity against human SW1736 cells after 96 hrs by SRB colorimetric assay
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[PMID: 20472329] |
In Vitro
NVX-207 induces cell death via apoptosis[1]. NVX-207 has a high cytotoxicity with IC50 values ranging from 7.6-8.5 μM, in the three analyzed malignant glioma cell lines. NVX-207 leads to PARP cleavage and to a decrease in Survivin expression levels under normoxic and hypoxic conditions. NVX-207 (20 μM) causes a significantly high rate of necrosis of glioma cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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. 745020-66-0
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Appearance Solid
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Masse moléculaire 601.86
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Formule C36H59NO6
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Color White to off-white
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SMILES
O=C([C@]1(CC[C@H]2C(C)=C)[C@@]2([H])[C@](CC[C@@]3([H])[C@]4(CC[C@]5([H])[C@@]3(CC[C@H](OC(C)=O)C5(C)C)C)C)([H])[C@@]4(C)CC1)OCC(CO)(N)CO
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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
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (207.69 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: ≥ 2.08 mg/mL (3.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Willmann M, et al. Characterization of NVX-207, a novel betulinic acid-derived anti-cancer compound. Eur J Clin Invest. 2009;39(5):384-394. [Content Brief]
[2]. Bache M, et al. Betulinic acid derivatives NVX-207 and B10 for treatment of glioblastoma--an in vitro study of cytotoxicity and radiosensitization. Int J Mol Sci. 2014 Oct 30;15(11):19777-90. [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 | 1.6615 mL | 8.3076 mL | 16.6152 mL | 41.5379 mL |
| 5 mM | 0.3323 mL | 1.6615 mL | 3.3230 mL | 8.3076 mL | |
| 10 mM | 0.1662 mL | 0.8308 mL | 1.6615 mL | 4.1538 mL | |
| 15 mM | 0.1108 mL | 0.5538 mL | 1.1077 mL | 2.7692 mL | |
| 20 mM | 0.0831 mL | 0.4154 mL | 0.8308 mL | 2.0769 mL | |
| 25 mM | 0.0665 mL | 0.3323 mL | 0.6646 mL | 1.6615 mL | |
| 30 mM | 0.0554 mL | 0.2769 mL | 0.5538 mL | 1.3846 mL | |
| 40 mM | 0.0415 mL | 0.2077 mL | 0.4154 mL | 1.0384 mL | |
| 50 mM | 0.0332 mL | 0.1662 mL | 0.3323 mL | 0.8308 mL | |
| 60 mM | 0.0277 mL | 0.1385 mL | 0.2769 mL | 0.6923 mL | |
| 80 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.5192 mL | |
| 100 mM | 0.0166 mL | 0.0831 mL | 0.1662 mL | 0.4154 mL |
NVX-207 Related Classifications
HY-101597 Related Classifications
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