Acrizanib是一种具有口服活性的血管内皮生长因子受体2（VEGFR-2）抑制剂。
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.
Acrizanib是一种具有口服活性的血管内皮生长因子受体2（VEGFR-2）抑制剂。Acrizanib可通过抑制VEGFR2的磷酸化来阻断血管生成信号通路。Acrizanib可用于年龄相关性黄斑变性和眼底新生血管性疾病的相关研究[1-2]。
在体外，Acrizanib（0-200nM）处理血管内皮生长因子（VEGF，10ng/mL）刺激的人脐静脉内皮细胞（HUVECs）24小时，Acrizanib可显著抑制VEGF诱导的细胞增殖、迁移及管形成能力[3]。Acrizanib（17.4nM）孵育BaF3-Tel-KDR细胞72小时，Acrizanib可显著抑制的细胞增殖[4]。
在体内，Acrizanib（0.5μL，10μM溶液玻璃体内注射）用于处理氧诱导视网膜病变小鼠模型。Acrizanib显著减少了病理性视网膜新生血管形成[3]。Acrizanib（4μL 1%混悬液/眼；每日三次；持续6天）用于处理激光诱导的Brown Norway大鼠脉络膜新生血管（CNV）模型。Acrizanib显著抑制了脉络膜新生血管面积[4]。
| 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 | |
| 别名 | 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 | ||
| 分子式 | C20H18F3N7O2 | 分子量 | 445.4 |
| 溶解度 | DMSO : 41.67 mg/mL (93.56 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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 |
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- Purity: >99.50% Appearance: A solid
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