Brivanib
Based on 2 publication(s) in Google Scholar
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
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- Pureza: 99.45%
- No. CAS: 649735-46-6
- Fòrmula: C19H19FN4O3
- Peso molecular:370.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) Brivanib
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Actividad biológica
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VEGFR2 25 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
618 nM
Compound: Brivanib, BMS-540215
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Inhibition of VEGF-stimulated HUVEC cell proliferation assessed as 5-bromo-2-deoxyuridine incorporation
Inhibition of VEGF-stimulated HUVEC cell proliferation assessed as 5-bromo-2-deoxyuridine incorporation
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[PMID: 22983304] |
| HUVEC | IC50 |
695 nM
Compound: Brivanib, BMS-540215
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Inhibition of FGF-stimulated HUVEC cell proliferation assessed as 5-bromo-2-deoxyuridine incorporation
Inhibition of FGF-stimulated HUVEC cell proliferation assessed as 5-bromo-2-deoxyuridine incorporation
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[PMID: 22983304] |
| HUVEC | IC50 |
841 nM
Compound: Brivanib, BMS-540215
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Inhibition of VEGF/FGF-stimulated HUVEC cell proliferation assessed as 5-bromo-2-deoxyuridine incorporation
Inhibition of VEGF/FGF-stimulated HUVEC cell proliferation assessed as 5-bromo-2-deoxyuridine incorporation
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[PMID: 22983304] |
Brivanib inhibits VEGFR1 and FGFR-1 with IC50 of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, brivanib exhibits low activity to tumor cell lines[1]. Brivanib doses ≤20 μM paradoxically enhances FGF-induced LX-2 cell proliferation, whereas higher brivanib doses (≥30 μM) inhibits LX-2 cell proliferation. The inhibitory effect of brivanib on liver fibrosis is not through inhibition of TGF-β1-induced stellate cell activation, and is possibly through inhibition of PDGF-BB-induced stellate cell activation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 649735-46-6
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Appearance Solid
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Peso molecular 370.38
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Fòrmula C19H19FN4O3
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Color White to light brown
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SMILES
FC1=C(OC2=NC=NN3C2=C(C(OC[C@H](O)C)=C3)C)C=CC4=C1C=C(C)N4
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Synonyms
BMS-540215
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Rep
Pharmacological boosting of cGAS activation sensitizes chemotherapy by enhancing antitumor immunity. [Abstract]2023 Mar 20;42(3):112275. PMID: 36943864
Brivanib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Mar 20;42(3):112275. [Abstract]
Brivanib (0.1, 1, 10 µM) markedly increases interactions of biotin-ISD with purified SUMO-cGAS in a dose-dependent manner, in Patient-derived tumor-like cell clusters (PTCs).
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (135.00 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: ≥ 2.08 mg/mL (5.62 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 (5.62 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.
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.
Protocolo
Viability is measured in LX-2 cells using the Cell Counting Kit-8 (CCK-8). Using 96-well plates with 2,000 cells per well, HSCs are incubated in 10% FBS-supplemented DMEM for 24 hours, followed by starvation in serum-free media. After 24 hours of starvation, brivanib is added at different doses. Two hours later, 5 ng/mL PDGF-BB is added. The cells are incubated for an additional 72 hours and cell viability is measured. Each experiment is performed in three replicates at least four times.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male mice 4-6 weeks of age are treated 3 times a week with a total of 12 intraperitoneal (i.p.) injections of 150 mL/kg TAA. At the onset of TAA treatment, placebo or brivanib (25 or 50 mg/kg) is administered orally on 5 consecutive days with weekend breaks. The animals are sacrificed 4 weeks after the start of the injections.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bhide RS, et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem, 2006, 49 (7), 2143-2146. [Content Brief]
[2]. Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res, 2008, [Content Brief]
[3]. Nakamura I, et al. Correction: Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF, VEGF and PDGF Signaling. PLoS One. 2015 Nov 3;10(11):e0142355. [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 | 2.6999 mL | 13.4997 mL | 26.9995 mL | 67.4987 mL |
| 5 mM | 0.5400 mL | 2.6999 mL | 5.3999 mL | 13.4997 mL | |
| 10 mM | 0.2700 mL | 1.3500 mL | 2.6999 mL | 6.7499 mL | |
| 15 mM | 0.1800 mL | 0.9000 mL | 1.8000 mL | 4.4999 mL | |
| 20 mM | 0.1350 mL | 0.6750 mL | 1.3500 mL | 3.3749 mL | |
| 25 mM | 0.1080 mL | 0.5400 mL | 1.0800 mL | 2.6999 mL | |
| 30 mM | 0.0900 mL | 0.4500 mL | 0.9000 mL | 2.2500 mL | |
| 40 mM | 0.0675 mL | 0.3375 mL | 0.6750 mL | 1.6875 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5400 mL | 1.3500 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4500 mL | 1.1250 mL | |
| 80 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8437 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6750 mL |
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