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Acrizanib

  Cat. No.:  DC11512   Featured
Chemical Structure
1229453-99-9
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More than 5000 active chemicals with high quality for research!
Field of application
Acrizanib（LHA510） is a potent and selective angiogenesis inhibitor and VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1229453-99-9
Chemical Name: Acrizanib
Synonyms: Acrizanib;F2CB8801I3;Acrizanib [INN];XPIHPLVWOUDMPF-UHFFFAOYSA-N;N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide;N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-(6-((methylamino)methyl)pyrimidin-4-yloxy)-1H-indole-1-carboxamide;1H-Indole-1-carboxamide, 5-((6-((methylamino)methyl)-4-pyrimidinyl)oxy)-N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-y
SMILES: FC(C1=C([H])C(=NN1C([H])([H])[H])N([H])C(N1C([H])=C([H])C2C([H])=C(C([H])=C([H])C1=2)OC1C([H])=C(C([H])([H])N([H])C([H])([H])[H])N=C([H])N=1)=O)(F)F
Formula: C20H18F3N7O2
M.Wt: 445.3978
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
Target: VEGFR-2:17.4 nM (IC50)
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].
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].
References: 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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC11512 Acrizanib Acrizanib（LHA510） is a potent and selective angiogenesis inhibitor and VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
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