Lucitanib
Based on 8 publication(s) in Google Scholar
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.94%
- CAS No.: 1058137-23-7
- Formule: C26H25N3O4
- Masse moléculaire:443.49
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Lucitanib
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Oncogene. 2023 Feb;42(6):434-448. [Abstract]
- Mol Cancer Ther. 2019 Jan;18(1):28-38. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Bioorg Chem. 2024 Jun:147:107412. [Abstract]
- bioRxiv. 2024 Jul 25.
- University of California. 2021 Sep.
Voir tous les produits spécifiques à Isoform VEGFR
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Activité biologique
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VEGFR1 7 nM (IC50) |
VEGFR2 25 nM (IC50) |
VEGFR3 10 nM (IC50) |
FGFR1 17.5 nM (IC50) |
FGFR2 82.5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-F10 | IC50 |
16.3 μM
Compound: 6
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Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 38870832] |
Consistent with the inhibitory activity of VEGFR and FGFR auto-phosphorylation, Lucitanib potently inhibits VEGF and bFGF-stimulated HUVEC proliferation with IC50 of 40 and 50 nM, respectively. Besides, Lucitanib (E-3810) also inhibits CSF-1R with IC50 of 5 nM[1]. Lucitanib potently inhibits FGFR2 activity (Ki<0.05 μM), follows by PDGFRα activity (Ki=0.11 μM). The Ki values obtained for DDR2, LYN, CARDIAK, CSBP (2), EPHA2, and YES range between 0.26 and 8 μM[2].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1058137-23-7
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Appearance Solid
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Masse moléculaire 443.49
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Formule C26H25N3O4
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Color White to yellow
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SMILES
O=C(NC)C1=CC=CC2=C1C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C43)=C2
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Synonyms
E-3810
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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 (8)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
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 -
Oncogene
2023 Feb;42(6):434-448. PMID: 36509998 -
Mol Cancer Ther
ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity. [Abstract]2019 Jan;18(1):28-38. PMID: 30301864 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
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Solvant et solubilité
DMSO : ≥ 20.83 mg/mL (46.97 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 (5.64 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 (5.64 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 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.
Protocole
Exponentially growing HUVEC or NHI3T3 cells are seeded into 96-well plates at a density of 3 to 6×103 cells/100 μL/well in complete medium. In the experiments without serum starvation, 24 hours after seeding, cells are exposed to different Lucitanib (E-3810) concentrations without or with VEGF165 (50 ng/mL) or bFGF (20 ng/mL) ligands and the antiproliferative effect of the drugs is evaluated after 72 hours by MTS Colorimetric Assay. In the assays with serum starvation conditions, 24 hours after seeding complete medium is removed and after 3 rounds of washing with PBS, cells are cultured in medium containing 1% BSA. After 18 to 24 hours, cells are processed. Exponentially growing A2780, A498, SN12KI, and HepG2 cells are seeded into 96-well plates at 3 to 5×103 cells/100 μL/well in complete medium. Twenty-four hours later cells are treated with different drug concentrations for 72 hours and the antiproliferative effect is evaluated by MTS[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
MDA-MB-231 tumor-bearing mice are randomized when their tumor masses are about 350 to 400 mg to receive Lucitanib (E-3810) (15 mg/kg), Brivanib, and SU 11248 at the doses used for the antitumor activity trial, for 10 days. Four hours after the antiangiogenic dose of day 7, NSC 125973 is injected intravenously at the dose of 20 mg/kg and tumor and plasma samples are collected after 1, 4, and 24 hours in all the groups (each group consisting of 3 animals). At the indicated sampling time, mice are anesthetized, blood is collected from the retro-orbital plexus into heparinized tubes, and the plasma fraction is separated. Mice are killed by cervical dislocation, and tumors excised and snap-frozen. The samples are analyzed by high-performance liquid chromatography (HPLC) with UV detection at 230 nm.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. [Content Brief]
[2]. Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. [Content Brief]
[3]. Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with NSC 125973 inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40 [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 | 2.2548 mL | 11.2742 mL | 22.5484 mL | 56.3711 mL |
| 5 mM | 0.4510 mL | 2.2548 mL | 4.5097 mL | 11.2742 mL | |
| 10 mM | 0.2255 mL | 1.1274 mL | 2.2548 mL | 5.6371 mL | |
| 15 mM | 0.1503 mL | 0.7516 mL | 1.5032 mL | 3.7581 mL | |
| 20 mM | 0.1127 mL | 0.5637 mL | 1.1274 mL | 2.8186 mL | |
| 25 mM | 0.0902 mL | 0.4510 mL | 0.9019 mL | 2.2548 mL | |
| 30 mM | 0.0752 mL | 0.3758 mL | 0.7516 mL | 1.8790 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5637 mL | 1.4093 mL |
Lucitanib Related Classifications
HY-15391 Related Classifications
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