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Acrizanib

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Catalog No. T5373Cas No. 1229453-99-9
Alias LHA510

Acrizanib (LHA510) is a VEGFR-2 inhibitor with an IC50 of 17.4 nM for BaF3-VEGFR-2.

Acrizanib

Acrizanib

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Purity: 99.64%
Catalog No. T5373Alias LHA510Cas No. 1229453-99-9
Acrizanib (LHA510) is a VEGFR-2 inhibitor with an IC50 of 17.4 nM for BaF3-VEGFR-2.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$113In StockIn Stock
5 mg$289In StockIn Stock
10 mg$446In StockIn Stock
25 mg$762In StockIn Stock
50 mg$1,060In StockIn Stock
100 mg$1,380-In Stock
1 mL x 10 mM (in DMSO)$318In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.64%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
Acrizanib (LHA510) is a VEGFR-2 inhibitor with an IC50 of 17.4 nM for BaF3-VEGFR-2.
Targets&IC50
VEGFR2:17.4 nM
In vitro
Acrizanib is a VEGFR-2 inhibitor with an IC50 of 17.4 nM for BaF3-KDR, and exhibits ≤10% remaining kinase activity against only 13 wild type kinases: CSF1R, Kit, PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, Fms (soluble VEGFR1), DDR1, DDR2, TIE1, and ABL1 (nonphosphorylated) [1].
In vivo
Rat ocular pharmacokinetic (PK) studies indicate that Acrizanib (compound 35) exhibits a notably different profile compared to compound 25, especially in terms of prolonged exposure within the posterior eye chamber (PEC). The area under the curve (AUC) ratio, reflecting Acrizanib's concentration in the PEC relative to its plasma levels, is significantly elevated, showing over 21000-fold higher exposure in the PEC compared to plasma by day 11. Additionally, Acrizanib demonstrates a substantially enhanced retina-to-plasma AUC exposure ratio after 10 days of administration (598× for Acrizanib versus 0.8× for compound 25)[1], distinctively unlike compound 25.
SynonymsLHA510
Chemical Properties
Molecular Weight445.4
FormulaC20H18F3N7O2
Cas No.1229453-99-9
SmilesCNCc1cc(Oc2ccc3n(ccc3c2)C(=O)Nc2cc(n(C)n2)C(F)(F)F)ncn1
Relative Density.1.47 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 37.8 mg/mL (84.87 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.49 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2452 mL11.2259 mL22.4517 mL112.2586 mL
5 mM0.4490 mL2.2452 mL4.4903 mL22.4517 mL
10 mM0.2245 mL1.1226 mL2.2452 mL11.2259 mL
20 mM0.1123 mL0.5613 mL1.1226 mL5.6129 mL
50 mM0.0449 mL0.2245 mL0.4490 mL2.2452 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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