Acrizanib 是一种 VEGFR-2 的抑制剂，其对 BaF3-VEGFR-2 的 IC50 值为 17.4 nM。

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

Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR. Acrizanib 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].

Rat ocular PK studies with Acrizanib (compound 35) 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)[1].

1229453-99-9

C20H18F3N7O2

445.40

LHA510

DMSO:37.8mg/mL (84.9mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years