Acrizanib

Modify Date: 2024-01-28 20:15:44

Acrizanib Structure
Acrizanib structure
Common Name Acrizanib
CAS Number 1229453-99-9 Molecular Weight 445.40
Density N/A Boiling Point N/A
Molecular Formula C20H18F3N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Acrizanib


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

 Names

Name Acrizanib

 Acrizanib Biological Activity

Description Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
Related Catalog
Target

VEGFR-2:17.4 nM (IC50)

In Vitro 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)[1].
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)[1].
References

[1]. Adams CM, et al. The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration. J Med Chem. 2018 Feb 22;61(4):1622-1635.

 Chemical & Physical Properties

Molecular Formula C20H18F3N7O2
Molecular Weight 445.40
Storage condition 2-8℃