| Identification | Back Directory | [Name]
Acrizanib | [CAS]
1229453-99-9 | [Synonyms]
LHA510
LHA 510
Acrizanib
LHA510;LHA 510
Acrizanib (LHA-510)
N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide
1H-Indole-1-carboxamide, 5-[[6-[(methylamino)methyl]-4-pyrimidinyl]oxy]-N-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]- | [Molecular Formula]
C20H18F3N7O2 | [MOL File]
1229453-99-9.mol | [Molecular Weight]
445.4 |
| Chemical Properties | Back Directory | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 41.67 mg/mL (93.56 mM) | [form ]
Solid | [pka]
10.53±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-VEGFR-2[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]. | [IC 50]
VEGFR-2: 17.4 nM (IC50) | [storage]
Store at -20°C | [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. DOI:10.1021/acs.jmedchem.7b01731 |
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