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Acrizanib

Chemical Structure : Acrizanib

CAS No.: 1229453-99-9

Acrizanib (LHA510;LHA 510)

Catalog No.: PC-60029Not For Human Use, Lab Use Only.

Acrizanib (LHA510, LHA-510) is a novel potent, selective VEGFR-2 (KDR) inhibitor with IC50 of 17.4 nM in cell-based assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Acrizanib (LHA510, LHA-510) is a novel potent, selective VEGFR-2 (KDR) inhibitor with IC50 of 17.4 nM in cell-based assays.
Acrizanib (LHA510) exhibits <10% remaining kinase activity against only 13 wildtype kinases, CSF1R, Kit, PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, Fms, DDR1, DDR2, TIE1, and ABL1 in a panel of >400 kinases.
Acrizanib (LHA510) demonstrates potency and efficacy in rodent CNV models, limited systemic exposure after topical ocular administration, multiple formulation options, and an acceptable rabbit ocular PK profile.

Physicochemical Properties

M.Wt 445.406
Formula C20H18F3N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-({6-[(methylamino)methyl]pyrimidin-4-yl}oxy)-N-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-1H-indole-1-carboxamide

References

1. Adams CM, et al. J Med Chem. 2018 Feb 5. doi: 10.1021/acs.jmedchem.7b01731.

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