Acrizanib
Based on 1 publication(s) in Google Scholar
Acrizanib (LHA510) is a small-molecule vascular endothelial growth factor receptor 2 (VEGFR-2, KDR) inhibitor. Acrizanib inhibits the proliferation of BaF3-Tel-KDR cells dependent on VEGFR-2 activity, with an IC50 of 17.4 nM. Acrizanib can be used in research related to choroidal neovascularization and neovascular age-related macular degeneration.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.84%
- CAS 番号: 1229453-99-9
- 分子式: C20H18F3N7O2
- 分子量:445.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Acrizanib
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生物活性
製品説明
IC50 & Target
[1]|
VEGFR-2 17.4 nM (IC50) |
体外実験
Acrizanib (LHA510) potently inhibits VEGFR-2-dependent proliferation of BaF3-Tel-KDR cells, with an IC50 of 17.4 nM[1].
Acrizanib (1 μM) exhibits residual kinase activity of ≤ 10% against only 13 wild-type kinases in a KINOMEscan screening targeting 442 kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFRα, PDGFRβ, KIT, DDR1, DDR2, and TIE1[1].
Acrizanib (1 μM; 0-30 min) has an RLM-derived Clint of 156 μL/min/mg in rat liver microsomal stability assays[1].
Acrizanib binds to synthetic melanin, with Bmax1 and Bmax2 values of 368 and 134 nmol/mg, respectively, and Kd1 and Kd2 values of 6.4 and 0.56 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Acrizanib (3% suspension; 4 μL/eye; topical ocular administration; bid) inhibits neovascular area by 94% in the laser-induced CNV model of Brown Norway rats[1].
Acrizanib (1% suspension; 4 μL/eye; topical ocular administration; tid) inhibits neovascular area by 90% in laser-induced CNV models of Brown Norway rats[1].
Dose-response experiments of Acrizanib in a laser-induced CNV model of Brown Norway rats show that the ED50 values for qd, bid and tid administration are 1.4%, 1.0% and 0.5%, respectively; the ED90 values for bid and tid administration are 2.6% and 1.2%, respectively, while the ED90 for qd administration is not determined[1].
Acrizanib (2% suspension; 30 μL; unilateral topical ocular administration; tid; 7 days) achieves sustained exposure in the retina and retinal pigment epithelium/choroid of pigmented New Zealand White × New Zealand Red F1 rabbits; based on an analysis of exposure differences between dosed and undosed eyes, the paper reports that 37% and 57% of the total AUC in the RPE/choroid and retina, respectively, are attributable to direct local delivery of the eye drops[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6[1]
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Dosage:3.5 μL × 1% suspension/eye
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Administration:topical ocular; three times a day; 5-7 days
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Result:Inhibited choroidal neovascular lesion area by 99%.
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Animal Model:Brown Norway[1]
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Dosage:3% suspension; 4 μL/eye
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Administration:Topical ocular administration to both eyes; bid
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Result:Inhibited neovascular area by 94%.
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Animal Model:Brown Norway rats; laser-induced choroidal neovascularization[1]
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Dosage:1% suspension; 4 μL/eye
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Administration:Topical ocular administration to both eyes; bid
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Result:Inhibited neovascular area by 90%.
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Animal Model:Brown Norway rats; laser-induced choroidal neovascularization[1]
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Dosage:Various formulation concentrations; 4 μL/eye
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Administration:Topical ocular administration; qd/bid/tid
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Result:Showed ED50 values of 1.4%, 1.0%, and 0.5% for qd, bid, and tid dosing and ED90 values of 2.6% and 1.2% for bid and tid dosing, respectively.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1229453-99-9
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性状 Solid
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分子量 445.40
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分子式 C20H18F3N7O2
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Color White to yellow
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SMILES
O=C(N1C2=CC=C(OC3=NC=NC(CNC)=C3)C=C2C=C1)NC4=NN(C)C(C(F)(F)F)=C4
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別名
LHA510
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Transl Vis Sci Technol
Acrizanib as a Novel Therapeutic Agent for Fundus Neovascularization via Inhibitory Phosphorylation of VEGFR2. [Abstract]2024 Jan 2;13(1):1. PMID: 38165719
溶剤 & 溶解度
体外:
DMSO : 41.67 mg/mL (93.56 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 2.08 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
純度とドキュメンテーション
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データシート (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Adams CM, 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. [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 | 2.2452 mL | 11.2259 mL | 22.4517 mL | 56.1293 mL |
| 5 mM | 0.4490 mL | 2.2452 mL | 4.4903 mL | 11.2259 mL | |
| 10 mM | 0.2245 mL | 1.1226 mL | 2.2452 mL | 5.6129 mL | |
| 15 mM | 0.1497 mL | 0.7484 mL | 1.4968 mL | 3.7420 mL | |
| 20 mM | 0.1123 mL | 0.5613 mL | 1.1226 mL | 2.8065 mL | |
| 25 mM | 0.0898 mL | 0.4490 mL | 0.8981 mL | 2.2452 mL | |
| 30 mM | 0.0748 mL | 0.3742 mL | 0.7484 mL | 1.8710 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5613 mL | 1.4032 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1226 mL | |
| 60 mM | 0.0374 mL | 0.1871 mL | 0.3742 mL | 0.9355 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7016 mL |
Acrizanib 関連分類
HY-109020 関連分類
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