Vorolanib
Based on 1 publication(s) in Google Scholar
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
For research use only. We do not sell to patients.
- Purity : 99.78%
- CAS No.: 1013920-15-4
- Formula: C23H26FN5O3
- Molecular Weight:439.48
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Vorolanib (Standard)Reference Standard
Publications Citing Use of MedChemExpress (MCE) Vorolanib
MoreAll VEGFR Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.0155 μM
Compound: CM082
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Cytotoxicity against HEK293 cells expressing ABCG2-R-482 wildtype assessed as decrease in mitoxantrone half inhibitory concentration
Cytotoxicity against HEK293 cells expressing ABCG2-R-482 wildtype assessed as decrease in mitoxantrone half inhibitory concentration
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[PMID: 35944339] |
| HEK293 | IC50 |
0.058 μM
Compound: CM082
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Cytotoxicity against HEK293 cells expressing ABCG2-R-482 mutant assessed as decrease in mitoxantrone half inhibitory concentration
Cytotoxicity against HEK293 cells expressing ABCG2-R-482 mutant assessed as decrease in mitoxantrone half inhibitory concentration
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[PMID: 35944339] |
| HUVEC | IC50 |
31.5 nM
Compound: CM082; X-82
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Inhibition of VEGF-induced HUVECs proliferation
Inhibition of VEGF-induced HUVECs proliferation
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[PMID: 37285684] |
In Vitro
Vorolanib (CM082; 1-100 μM) can specifically enhance the sensitivity of a substrate chemotherapeutical agent in overexpressing ABCG2 cells, but not in overexpressing ABCB1 cells. Vorolanib (1.25, 2.5, 5.0, 20 μM) does not influence the expression of ABCG2 in mRNA or protein Levels[1].
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Vorolanib (0.001-10 μM) inhibits the growth of VEGF‐stimulated HUVECs (IC50=0.031 μM) and FBS‐stimulated HUVEC growth (IC50=29.9?μM)[2].
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Vorolanib (0.01, 0.1, 1 μM) exhibits a concentration‐dependent inhibition on VEGF‐induced (40 ng/mL) phosphorylation of VEGFR2 and its downstream signaling molecules ERK1/2, AKT, and STAT3 in HUVECs. Vorolanib (0.1, 1 μM) inhibits FBS‐stimulated tube formation and cell migration of HUVECs in a concentration‐dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
? Vorolanib (80 mg/kg; twice daily; for 21 days) has antitumor activity combined with ZD1839 (10 mg/kg; q.d; for 21 days) on H3255 tumor xenograft (female BALB/c nude mice aged five weeks)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1013920-15-4
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Appearance Solid
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Molecular Weight 439.48
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Formula C23H26FN5O3
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Color Light yellow to yellow
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SMILES
O=C1/C(C2=CC(F)=CC=C2N1)=C/C(NC(C)=C3C(N[C@@H]4CN(C(N(C)C)=O)CC4)=O)=C3C
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Synonyms
CM082; X-82
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 27 mg/mL (61.44 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: ≥ 2.25 mg/mL (5.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
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.
Protocols
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Human pluripotent stem cell endothelial-cell differentiation
Human pluripotent stem cell endothelial differentiation is based on stepwise developmental patterning: early activation of WNT/GSK3β inhibition promotes mesodermal or vascular progenitor entry, followed by endothelial specification using VEGF-related signaling, BMP4, FGF2, Notch modulation, or cAMP depending on the published protocol. Endothelial differentiation is read out by acquisition of CD31, CD34, VE-cadherin/CD144, KDR/VEGFR2, vWF, Tie2, NOS3, acetylated LDL uptake, tube/network formation, barrier function, and in vivo vessel-forming capacity where tested.
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Vascular/Branching Fractal Analysis
Vascular/branching fractal analysis quantifies the geometric complexity of vessel trees or vascular networks from segmented 2D images, commonly by converting vessels into binary and/or skeletonized maps and estimating fractal dimension using box-counting or related approaches. Fractal dimension is interpreted as an image-derived readout of vascular branching complexity, space filling, or density, and has been applied to retinal photographs, fluorescein angiography, OCT angiography, capillary perfusion maps, and in vitro Matrigel angiogenesis networks. The assay readout is generated from vessel-positive pixels after image preprocessing, vessel segmentation, binarization, and optional skeletonization; reported outputs include fractal dimension, vessel density, branchpoint density, endpoint density, vessel length density, tortuosity, and generation-based branching metrics when VESGEN-style analysis is used. The biological interpretation is limited to quantitative vascular patterning and s
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Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Endothelial Cell Migration/Angiogenic Sprouting Assay
Endothelial cell migration and angiogenic sprouting assays are in vitro (and partially ex vivo-adapted) functional models that quantify the ability of endothelial cells to undergo coordinated migration, extracellular matrix invasion, and multicellular organization into capillary-like sprouts in response to pro-angiogenic stimuli such as VEGF, bFGF, or conditioned microenvironments. These assays are used to model early angiogenic events including tip-cell formation, directional migration, and lumen-like sprout extension, which collectively reflect angiogenic activation and vascular morphogenesis processes observed in vivo.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Lejia Xu, et al. CM082 Enhances the Efficacy of Chemotherapeutic Drugs by Inhibiting the Drug Efflux Function of ABCG2. Mol Ther Oncolytics. 2019 Dec 27;16:100-110. [Content Brief]
[2]. Kun Zhang, et al. CM082, a novel angiogenesis inhibitor, enhances the antitumor activity of ZD1839 on epidermal growth factor receptor mutant non-small cell lung cancer in vitro and in vivo. Thorac Cancer. 2020 Jun;11(6):1566-1577. [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 | 2.2754 mL | 11.3771 mL | 22.7542 mL | 56.8854 mL |
| 5 mM | 0.4551 mL | 2.2754 mL | 4.5508 mL | 11.3771 mL | |
| 10 mM | 0.2275 mL | 1.1377 mL | 2.2754 mL | 5.6885 mL | |
| 15 mM | 0.1517 mL | 0.7585 mL | 1.5169 mL | 3.7924 mL | |
| 20 mM | 0.1138 mL | 0.5689 mL | 1.1377 mL | 2.8443 mL | |
| 25 mM | 0.0910 mL | 0.4551 mL | 0.9102 mL | 2.2754 mL | |
| 30 mM | 0.0758 mL | 0.3792 mL | 0.7585 mL | 1.8962 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5689 mL | 1.4221 mL | |
| 50 mM | 0.0455 mL | 0.2275 mL | 0.4551 mL | 1.1377 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9481 mL |
Vorolanib Related Classifications
HY-109019 Related Classifications
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