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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 | Availability | Quantity |
---|---|---|---|
1 mg | $113 | In Stock | |
5 mg | $289 | In Stock | |
10 mg | $446 | In Stock | |
25 mg | $762 | In Stock | |
50 mg | $1,060 | In Stock | |
100 mg | $1,380 | In Stock | |
1 mL x 10 mM (in DMSO) | $318 | In Stock |
Description | Acrizanib (LHA510) is a VEGFR-2 inhibitor with an IC50 of 17.4 nM for BaF3-VEGFR-2. |
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. |
Alias | 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. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 37.8 mg/mL (84.9 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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