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Axitinib 阿西替尼;阿昔替尼

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Axitinib是一种多靶点抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3,PDGFR-β和c-KIT时,其IC50分别为0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM和1.7 nM。

Axitinib结构式

别名:AG-013736

包装 价格 库存状态
Free Sample (0.5-1 mg)  原价 ¥ 0
促销价 ¥ 0
中国库存现货
10mM*1mL in DMSO 原价 ¥ 600
促销价 ¥ 570
中国库存现货
50mg 原价 ¥ 540
促销价 ¥ 513
中国库存现货
100mg 原价 ¥ 840
促销价 ¥ 798
中国库存现货
200mg 原价 ¥ 1080
促销价 ¥ 1026
中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Axitinib是一种多靶点抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3,PDGFR-β和c-KIT时,其IC50分别为0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM和1.7 nM。Axitinib是受体激酶抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3, PDGFR-β和c-KIT时IC50分别为0.1 , 0.2, 0.1-0.3, 1.6 和1.7 nM 。Axitinib可以阻断VEGFR的自磷酸化作用,VEGF调节的内皮细胞活力,微管形成,及下游信号。Axitinib抑制多种细胞系的增殖,如作用于IGR-N91, IGR-NB8, SH-SY5Y ,无VEGF刺激的HUVEC时IC50分别为>1000 nM, 849 nM, 274 nM和573 nM。

使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Int J Cancer (2017) . Figure 6. Axitinib (20 mg/kg, Abmole Bioscience)
方法
细胞系/动物模型 Hmga2/T mice
浓度 20mg/kg
处理时间 6 weeks
实验结果 Together, these results show that, while bromocriptine and/or axitinib were able to correct structuralabnormalities of tumoral vessels with a similar efficacy, only the combination treatment restored their function.
数据来源 Int J Cancer (2017) . Figure 5. Axitinib (20 mg/kg, Abmole Bioscience)
方法
细胞系/动物模型 Hmga2/T mice
浓度 20mg/kg
处理时间 6 weeks
实验结果 Analysis of pituitary vasculature in various conditions and morphometric measurements of blood vessels demonstrate that D2R agonist or axitinib had an equivalent capacity to improve structural defects present in tumoral blood vessels and that the combination treatment did not lead to a significant advantage.
数据来源 Int J Cancer (2017) . Figure 4. Axitinib (20 mg/kg, Abmole Bioscience)
方法
细胞系/动物模型 Hmga2/T mice
浓度 20mg/kg
处理时间 6 weeks
实验结果 Importantly, the expression of Angpt1 and Prok1, which was upregulated in response to bromocriptine treatment, was unchanged and remained low after axitinib treatment (Fig. 4d).
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines
方法 MTS cell proliferation assay
HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines were seeded at 5,000 cells per well in a 96-well plate and left to settle overnight in EMBV R-2 or DMEM with 10% fetal calf serum. The cells were treated with axitinib at concentrations ranging from 1 nmol/l to 10 lmol/l. Cell viability was determined after 72 hr using MTS tetrazolium substrate (CellTiter 96 Aqueous One Solution Cell Proliferation Assay; Promega Corporation, Charbonnieres, France) and colorimetric measurement at 490 nm in an automatic plate reader (Elx808; Fisher Bioblock Scientific SAS, Illkirch, France). IC50 values were calculated using GraphPadV R Prism software (version 3.00).
浓度 1 nM - 10 μM
处理时间 72 hr
动物实验
动物模型 IGR-N91 xenografts with female SPF-Swiss athymic nude mice at 6–8 weeks of age
配制 0.5% CMC
剂量 30 mg/kg BID for 2 weeks
给药处理 oral gavage
化学数据
分子量 386.47
分子式 C22H18N4OS
CAS号 319460-85-0
溶解性(25°C) DMSO ≥ 20 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

以下数据基于产品分子量,对于具体产品,请根据在不同溶剂中的溶解度和COA中的说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.5875 mL 12.9376 mL 25.8752 mL
5 mM 0.5175 mL 2.5875 mL 5.175 mL
10 mM 0.2588 mL 1.2938 mL 2.5875 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Carmichael et al. Clin Adv Hematol Oncol. Comprehensive overview of axitinib development in solid malignancies: focus on metastatic renal cell carcinoma.

[2] Pithavala et al. Cancer Chemother Pharmacol. Evaluation of the effect of food on the pharmacokinetics of axitinib in healthy volunteers.

[3] Jochen Rössler, et al. Int J Cancer. The selective VEGFR1-3 inhibitor axitinib (AG-013736) shows antitumor activity in human neuroblastoma xenografts

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关键词:Axitinib, AG-013736, Axitinib供应商, VEGFR/PDGFR抑制剂, 购买Axitinib, Axitinib溶解度, Axitinib结构式








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