NBM-T-BMX-OS01
Based on 1 Customer Validation
NBM-T-BMX-OS01 (BMX) is a derivative of Osthole (HY-N0054). NBM-T-BMX-OS01 attenuates the phosphorylation levels of ERK and Akt in an AMPK-dependent manner. NBM-T-BMX-OS01 induces oxidative stress through the production of ROS. NBM-T-BMX-OS01 enhances Cisplatin-induced cell proliferation inhibition, colony formation inhibition, apoptosis (apoptosis) and cell cycle arrest. NBM-T-BMX-OS01 inhibits VEGF-induced phosphorylation of VEGFR2 and FAK. NBM-T-BMX-OS01 inhibits VEGF-induced endothelial cell proliferation, migration and tube formation, as well as microvessel sprouting in rat aortic rings and angiogenesis induced by colorectal cancer cells. NBM-T-BMX-OS01 inhibits the growth of subcutaneous colorectal cancer xenografts in nude mice. NBM-T-BMX-OS01 can be used in studies related to lung cancer, colorectal cancer and angiogenesis.
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- Pureté : 99.74%
- CAS No.: 1246952-34-0
- Formule: C23H27NO5
- Masse moléculaire:397.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Activité biologique
Description
IC50 & Target
[2]|
VEGFR2 |
In Vitro
NBM-T-BMX-OS01 (1 μM; 14 days) enhances the Cisplatin-induced reduction in clonogenic survival rate of A549 cells[1].
NBM-T-BMX-OS01 (1-10 μM; 24-28 h) reduces the cell viability of HCT116 in a time- and concentration-dependent manner and inhibits serum-induced proliferation[2].
NBM-T-BMX-OS01 (1-5 μM; 24 h) regulates the levels of cell cycle regulatory proteins in HCT116, upregulating p21cip/Waf1 and downregulating survivin[2].
NBM-T-BMX-OS01 (1-5 μM; 16 h) inhibits VEGF-induced migration and capillary tube formation of HUVECs in a concentration-dependent manner[2].
NBM-T-BMX-OS01 (1-5 μM; 30 min pre-treatment followed by 5 or 30 min VEGF stimulation) concentration-dependently inhibits VEGF-induced activation of VEGFR2 and the activation of downstream signaling kinases (Src, FAK, Akt, ERK1/2) in HUVECs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human lung cancer A549 cells, normal bronchial HBE cells
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Concentration:0.1, 0.5, 1, 5, 10 μM
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Incubation Time:24 h
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Result:Significantly reduced cell viability in A549 cells at 5 μM and 10 μM.
Caused no obvious toxicity in HBE cells at all tested concentrations.
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Cell Line:human lung cancer A549 cells (in combination with cisplatin)
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Concentration:0.5, 1, 5 μM (pre-incubation before 10 μM cisplatin treatment); 1 μM (pre-incubation before 10 μM cisplatin treatment)
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Incubation Time:24 h total incubation; 12, 24, 48, 72 h total incubation
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Result:Significantly decreased cell viability compared to cisplatin treatment alone at 0.5 μM after 24 h.
Enhanced cisplatin-induced cell viability reduction in a time-dependent manner up to 72 h at 1 μM, with progressively lower cell viability at each time point compared to cisplatin alone.
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Cell Line:human lung cancer A549 cells (in combination with cisplatin)
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Concentration:1 μM (in combination with 10 μM cisplatin)
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Incubation Time:24 h
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Result:Significantly increased the number of TUNEL-positive apoptotic cells compared to cisplatin alone.
Enhanced cisplatin-induced caspase-3 activation compared to cisplatin alone.
Increased the apoptotic rate (without affecting necrosis) compared to cisplatin alone.
Caused accumulation of cells in the subG1 phase and a reduction in the G2/M phase fraction.
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Cell Line:human umbilical vascular endothelial cells (HUVECs) stimulated with vascular endothelial growth factor (VEGF)
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Concentration:1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:24 h (following 30 min pre-treatment)
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Result:Concentration-dependently reduced cell viability in VEGF-stimulated HUVECs.
Caused statistically significant decreases in cell viability at 5 μM and 10 μM compared to VEGF-only treated cells.
Did not significantly increase lactate dehydrogenase (LDH) release at 10 μM for 24 h, indicating no cytotoxic effect.
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Cell Line:human umbilical vascular endothelial cells (HUVECs) stimulated with vascular endothelial growth factor (VEGF)
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Concentration:1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:24 h (following 30 min pre-treatment)
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Result:Concentration-dependently inhibited VEGF-induced HUVEC proliferation, with statistically significant decreases observed at all tested concentrations compared to VEGF-only treated cells.
Did not cause significant increase in early or late apoptotic/necrotic cells as revealed by flow cytometric analysis with annexin V-FITC and propidium iodide.
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Cell Line:human umbilical vascular endothelial cells (HUVECs) stimulated with vascular endothelial growth factor (VEGF)
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Concentration:1 μM, 2 μM, 5 μM
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Incubation Time:16 h
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Result:Concentration-dependently reduced the number of VEGF-induced migrated HUVECs, with statistically significant decreases observed at all tested concentrations compared to VEGF-only treated cells.
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Cell Line:human umbilical vascular endothelial cells (HUVECs) stimulated with vascular endothelial growth factor (VEGF)
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Concentration:1 μM, 2 μM, 5 μM
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Incubation Time:30 min pre-treatment followed by 5 min (VEGFR2, Src) or 30 min (FAK, Akt, ERK1/2) VEGF stimulation
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Result:Concentration-dependently inhibited VEGF-induced phosphorylation of VEGFR2 at tyrosine residues 1175 and 1214, Src at tyrosine 416, FAK at tyrosine 397, Akt at serine 473, and ERK1/2 at threonine 202/tyrosine 204 (ERK1) and threonine 185/tyrosine 187 (ERK2), with statistically significant decreases observed at all tested concentrations compared to VEGF-only treated cells.
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Cell Line:human umbilical vascular endothelial cells (HUVECs)
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Concentration:1 μM, 2 μM, 5 μM
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Incubation Time:24 h
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Result:Concentration-dependently increased p21cip/Waf1 protein levels and decreased cyclinD1, CDK4, and survivin protein levels, with statistically significant changes observed at 2 μM and 5 μM for all proteins compared to untreated control cells.
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Cell Line:HCT116 human colorectal cancer cells
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Concentration:1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:24 h, 28 h; 24 h (in serum-containing medium following 24 h serum starvation)
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Result:Decreased HCT116 cell viability in a time- and concentration-dependent manner, with statistically significant decreases observed at 5 μM and 10 μM after 24 h, and at 5 μM and 10 μM after 28 h.
Concentration-dependently inhibited serum-induced HCT116 proliferation, with significant decreases observed at 5 μM and 10 μM compared to serum-only treated cells.
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Cell Line:HCT116 human colorectal cancer cells
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Concentration:1 μM, 2 μM, 5 μM
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Incubation Time:24 h
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Result:Concentration-dependently increased p21cip/Waf1 protein levels and decreased survivin protein levels, with statistically significant changes observed at 2 μM and 5 μM compared to untreated control cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude nu/nu (3-5 weeks old)[2]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 10 days/22 days
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Result:Reduced neovascularization (pale color compared to vehicle-treated controls).
Decreased microvessel density via CD31 immunohistochemical staining.
Markedly reduced hemoglobin content relative to vehicle-treated controls.
Significantly reduced tumor volumes compared to vehicle-treated controls.
Significantly lowered tumor weights compared to vehicle-treated controls.
Showed no significant difference in body weight relative to vehicle-treated controls.
- Human pluripotent stem cell endothelial-cell differentiation
- Cell migration
- Somatic Cell Culture
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Endothelial Tube Formation Assay
- Apoptosis Solutions
- Soft Agar Colony Formation Assay
- MTT Cell Proliferation Assay
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Western Blot
- Vascular/Branching Fractal Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- How to Select the Route of Administration for Mammals
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Protocol for Kinase activity and phosphorylation assays
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1246952-34-0
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Appearance Solid
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Masse moléculaire 397.46
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Formule C23H27NO5
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Color Light yellow to yellow
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SMILES
COC(C=C1)=CC=C1COC2=C(C(OC)=CC=C2/C=C/C(NO)=O)C/C=C(C)\C
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Synonyms
BMX
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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 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (251.60 mM; Need warming; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.29 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 (6.29 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). 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.
Pureté et documentation
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Fiche technique (290 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chen TJ, et al. NBM-T-BMX-OS01, an Osthole Derivative, Sensitizes Human Lung Cancer A549 Cells to Cisplatin through AMPK-Dependent Inhibition of ERK and Akt Pathway. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2015;36(3):893-906. [Content Brief]
[2]. Yang HY, et al. Anti-cancer activity of an osthole derivative, NBM-T-BMX-OS01: targeting vascular endothelial growth factor receptor signaling and angiogenesis. PloS one. 2013;8(11):e81592. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5160 mL | 12.5799 mL | 25.1598 mL | 62.8994 mL |
| 5 mM | 0.5032 mL | 2.5160 mL | 5.0320 mL | 12.5799 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5160 mL | 6.2899 mL | |
| 15 mM | 0.1677 mL | 0.8387 mL | 1.6773 mL | 4.1933 mL | |
| 20 mM | 0.1258 mL | 0.6290 mL | 1.2580 mL | 3.1450 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0064 mL | 2.5160 mL | |
| 30 mM | 0.0839 mL | 0.4193 mL | 0.8387 mL | 2.0966 mL | |
| 40 mM | 0.0629 mL | 0.3145 mL | 0.6290 mL | 1.5725 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2580 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4193 mL | 1.0483 mL | |
| 80 mM | 0.0314 mL | 0.1572 mL | 0.3145 mL | 0.7862 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6290 mL |
NBM-T-BMX-OS01 Related Classifications
HY-176498 Related Classifications
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Keywords
- NBM-T-BMX-OS01
- 1246952-34-0
- BMX
- VEGFR
- FAK
- Akt
- PERK
- AMPK
- Reactive Oxygen Species (ROS)
- Apoptosis
- Vascular endothelial growth factor receptor
- PTK2 protein tyrosine kinase 2
- PTK2
- Focal adhesion kinase
- PKB
- Protein kinase B
- Protein kinase R-like endoplasmic reticulum kinase
- PKR-like endoplasmic reticulum kinase
- AMP-activated protein kinase
- angiogenesis
- VEGFR2
- apoptosis
- human umbilical vascular endothelial cells (HUVECs)
- ERK
- human lung cancer A549 cells
- HCT116 human colorectal cancer cells
- reactive oxygen species
- Inhibitor
- inhibitor
- inhibit