Acrizanib (Synonyms: LHA510) |
Catalog No.GC30242
One-Click Copy Product Info
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Acrizanib is an orally active vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1229453-99-9
Sample solution is provided at 25 µL, 10mM.
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Acrizanib is an orally active vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitor. Acrizanib blocks the angiogenesis signaling pathway by inhibiting the phosphorylation of VEGFR2. Acrizanib is applicable in research related to age-related macular degeneration and fundus neovascular diseases[1-2].
In vitro, Acrizanib (0-200nM) was used to treat human umbilical vein endothelial cells (HUVECs) stimulated with vascular endothelial growth factor (VEGF, 10ng/mL) for 24 hours. Acrizanib significantly inhibited VEGF-induced cell proliferation, migration, and tube formation ability[3]. After incubating BaF3-Tel-KDR cells with Acrizanib (17.4nM) for 72 hours, Acrizanib significantly inhibited cell proliferation[4].
In vivo, Acrizanib (0.5μL, 10μM solution intravitreal injection) was used to treat a mouse model of oxygen-induced retinopathy. Acrizanib significantly reduced pathological retinal neovascularization[3]. In a laser-induced choroidal neovascularization (CNV) model in Brown Norway rats, Acrizanib (4μL of 1% suspension/eye; three times daily; for 6 days) was administered. Acrizanib significantly inhibited the area of choroidal neovascularization[4].
References:
[1] Al-Khersan H, Hussain RM, Ciulla TA, et al. Innovative therapies for neovascular age-related macular degeneration. Expert Opin Pharmacother. 2019 Oct;20(15):1879-1891.
[2] Hussain RM, Ciulla TA. Emerging vascular endothelial growth factor antagonists to treat neovascular age-related macular degeneration. Expert Opin Emerg Drugs. 2017 Sep;22(3):235-246.
[3] Tang X, Cui K, Wu P, et al. Acrizanib as a Novel Therapeutic Agent for Fundus Neovascularization via Inhibitory Phosphorylation of VEGFR2. Transl Vis Sci Technol. 2024 Jan 2;13(1):1.
[4] Adams CM, Anderson K, Artman G 3rd, et al. The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration. J Med Chem. 2018 Feb 22;61(4):1622-1635.
| Cell experiment [1]: | |
Cell lines | Engineered BaF3-Tel-KDR cells (survival is dependent on VEGFR-2 kinase domain activity) |
Preparation Method | The cells are engineered to constitutively require VEGFR-2 kinase domain activity for survival. The assay measures the inhibition of cell proliferation by Acrizanib (0-200nM; 72h). |
Reaction Conditions | 0-200nM; 72h. |
Applications | Acrizanib inhibited the proliferation of BaF3-Tel-KDR cells with a half-maximal inhibitory concentration (IC50) of 17.4nM. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Mother mice and their neonatal pups were exposed to 75% ± 5% O2 at postnatal day 7 (P7) and returned to room air (21% O2) at P12. Mice received an intravitreal injection of Acrizanib (0.5µL of 10µM solution) or vehicle at P12 and were euthanized for sample collection at P17. |
Dosage form | 0.5µL of 10µM solution; Intravitreal injection; Single injection at P12. |
Applications | Acrizanib significantly reduced pathological retinal neovascularization and the central avascular area. Acrizanib also reduced vascular leakage and inflammation (infiltration of microglia/macrophages and leukocytes, and levels of TNF-α and IL-1β) associated with neovascularization. |
References: | |
| Cas No. | 1229453-99-9 | SDF | |
| Synonyms | LHA510 | ||
| Canonical SMILES | O=C(N1C2=CC=C(OC3=NC=NC(CNC)=C3)C=C2C=C1)NC4=NN(C)C(C(F)(F)F)=C4 | ||
| Formula | C20H18F3N7O2 | M.Wt | 445.4 |
| Solubility | DMSO : 41.67 mg/mL (93.56 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2452 mL | 11.2259 mL | 22.4517 mL |
| 5 mM | 449 μL | 2.2452 mL | 4.4903 mL |
| 10 mM | 224.5 μL | 1.1226 mL | 2.2452 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)