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编 号:F083847
分子式:C20H18F3N7O2
分子量:445.4
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-VEGFR-2.

体内研究:
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).

体外研究:
Acrizanib is a VEGFR-2 inhibitor, with an IC50 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).
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