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CAS No.: 1229453-99-9

Acrizanib Catalog No. CSN23877

Synonyms: LHA510

Acrizanib is a selective VEGFR2 inhibitor with IC50 value of 17.4nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Acrizanib is a selective VEGFR2 inhibitor with IC50 value of 17.4nM, which can be used through topical ocular administration and multiple formulation options with potency and efficacy in rodent choroidal neovascularization models. Administration of Acrizanib through 1% suspension in volume of 3.5μl/eye tid could inhibit choroidal neovascularization to 99% in mice. The choroidal neovascularization in rats could be inhibited by 94% through 3% suspension in volume of 4μl/eye tid, bid. Topical administration of Acrizanib facilitates the limit of systemic exposure and as a therapy for neovascular agerelated macular degeneration.

动物研究

剂量

Cynomolgus monkey: 30 μl× 1% suspension/eye (topical ocular dosing, TID)

给药途径

Ocular dosing

动物药代数据

Animal	Monkeys^[1]
Dose	30 μl × 1.0%
Administration	ocular administration to each eye
T_1/2	1.61 h (solution) 4.38 h (suspension)
T_max	0.67 h (solution) 1.67 h (suspension)
C_max	26.9 nM (solution) 5.38 nM (suspension)
AUC_0→6h	64.4 nM·h (solution) 22.7 nM·h (suspension)

参考文献

[1] Adams CM, Anderson K, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2452 mL
- 11.2259 mL
- 22.4517 mL
- 5 mM
- 0.4490 mL
- 2.2452 mL
- 4.4903 mL
- 10 mM
- 0.2245 mL
- 1.1226 mL
- 2.2452 mL

技术信息

CAS号

1229453-99-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H18F3N7O2

运输

蓝冰

分子量

445.40

别名

LHA510

溶解度

DMSO	40.0 mg/mL (89.8 mM) warming

动物实验配方

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