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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $113 | In Stock | In Stock | |
| 5 mg | $289 | In Stock | In Stock | |
| 10 mg | $446 | In Stock | In Stock | |
| 25 mg | $762 | In Stock | In Stock | |
| 50 mg | $1,060 | In Stock | In Stock | |
| 100 mg | $1,380 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $318 | In Stock | In Stock |
| 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. |
| Synonyms | LHA510 |
| Molecular Weight | 445.4 |
| Formula | C20H18F3N7O2 |
| Cas No. | 1229453-99-9 |
| Smiles | CNCc1cc(Oc2ccc3n(ccc3c2)C(=O)Nc2cc(n(C)n2)C(F)(F)F)ncn1 |
| Relative Density. | 1.47 g/cm3 (Predicted) |
| Storage | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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