GLPBio

Acrizanib

Catalog No.: GC30242Purity:>99.50%Synonyms: LHA510
COASDSData Sheet
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.

Acrizanib
Cas No.: 1229453-99-9
10mM (in 1mL DMSO)In Stock
$192.00
1
1mgIn Stock
$78.00
1
5mgIn Stock
$196.00
1
10mgIn Stock
$302.00
1
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Description

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.

Protocol

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:
[1] 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.
[2] 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1229453-99-9
Synonyms
LHA510
SMILES
O=C(N1C2=CC=C(OC3=NC=NC(CNC)=C3)C=C2C=C1)NC4=NN(C)C(C(F)(F)F)=C4
Molecular Formula
C20H18F3N7O2
Molecular Weight
445.4
Solubility
DMSO : 41.67 mg/mL (93.56 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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