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Acrizanib (Synonyms: LHA510)

Katalog-Nr.GC30242

Acrizanib (LHA510) ist ein VEGFR-2-Inhibitor mit einem IC50-Wert von 17,4 nM fÜr BaF3-VEGFR-2.

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Acrizanib Chemische Struktur

Cas No.: 1229453-99-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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

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].

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].

[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 Properties

Cas No. 1229453-99-9 SDF
Überlieferungen LHA510
Canonical SMILES O=C(N1C2=CC=C(OC3=NC=NC(CNC)=C3)C=C2C=C1)NC4=NN(C)C(C(F)(F)F)=C4
Formula C20H18F3N7O2 M.Wt 445.4
Löslichkeit DMSO : 41.67 mg/mL (93.56 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2452 mL 11.2259 mL 22.4517 mL
5 mM 0.449 mL 2.2452 mL 4.4903 mL
10 mM 0.2245 mL 1.1226 mL 2.2452 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 14 reference(s) in Google Scholar.)

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