Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC 50 of 17.4 nM for BaF3-VEGFR-2
In Vitro
Acrizanib is a VEGFR-2 inhibitor, with an IC 50 of 17.4 nM for BaF3-KDR. Acrizanib (compound 35) 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Rat ocular PK studies with Acrizanib shows a distinctly different profile from that observed with compound 25. While prolonged exposure is once again evident in the PEC, the AUC ratio to the level of Acrizanib in plasma is markedly increased (>21000-fold higher exposure in the PEC than plasma on day 11). Furthermore, unlike 25, Acrizanib also afford much improved retina to plasma AUC exposure ratio after 10 days of dosing (598× for Acrizanib vs 0.8× for 25) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:VEGFR-2 17.4 nM (IC 50 )
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