阿昔替尼|T1452

Axitinib
319460-85-0

￥328 25mg 起订

￥465 50mg 起订

￥751 100mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 阿昔替尼

英文名称：: Axitinib

CAS号：: 319460-85-0

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature,keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.81%

产品类别：: 抑制剂

货号：: T1452

Product Introduction

Bioactivity

名称	Axitinib
描述	Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.
细胞实验	Endothelial or tumor cells were starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib was added and cells were incubated for 45 min at 37°C in the presence of 1 mmol/L Na3VO4. The appropriate growth factor was added to the cells, and after 5 min, cells were rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates were incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes were conjugated to protein A beads and supernatants were separated by SDS-PAGE. The Super Signal West Dura kit was used to detect the chemiluminescent signal [1].
激酶实验	Porcine aorta endothelial (PAE) cells overexpressing full-length VEGFR-2, PDGFR-β, KIT, and NIH-3T3 overexpressing murine VEGFR-2 (Flk-1) or PDGFR-α were generated as described previously. The ELISA capture plates were prepared by coating 96-well ReactiBind plates with 100 μL/well of 2.5 μg/mL anti-VEGFR-2 antibody, 0.75 μg/mL anti-PDGFR-β antibody, 0.25 μg/mL anti-PDGFR-α antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody. Measurement of RTK phosphorylation by ELISA was done as described previously [1].
动物实验	AG-013736, a receptor kinase inhibitor of VEGFRs and, at higher doses, PDGFRs (IC50 = 0.1 nmol/L for VEGFR-1, 0.2 nmol/L for VEGFR-2, 0.1–0.3 nmol/L for VEGFR-3, and 1.6 nmol/L for PDGFRβ; ref. 18), was provided by Pfizer Global Research and given once daily by gavage in a volume of 0.13 mL. Control animals received 0.5% carboxymethylcellulose drug carrier. Irradiations were done on nonanesthetized mice using a 137Cs source operating at 2.4 Gy/min. Mice were confined to plastic jigs with tumor-bearing legs extended through an opening in the side, allowing local irradiations. Fractionated doses were given in five daily 2 Gy fractions per week (omitting weekends). For combination treatments, radiotherapy was delivered first, and AG-013736 was given within ～4 h. Mice were sacrificed, and tumors were excised and then quick frozen (using liquid nitrogen) following 1, 2, or 3 weeks of treatment [3].
体外活性	方法：胶质瘤细胞 U87、T98 和 U251 用 Axitinib (0.1-100 µM) 处理 72 h，通过 MTT assay 测定细胞活力。结果：治疗 72 h 后，Axitinib 抑制 U87 和 T98 细胞的生长，IC50 值分别为 12.7 µM 和 8.5 µM。相反，U251 细胞对 Axitinib 介导的细胞毒性作用更具抵抗力。[1] 方法：人上皮卵巢癌细胞 A2780、RMG1、HeyA8 和 HeyA8-MDR 用 Axitinib (1-4 µM) 处理 4 h，通过 Western Blot 检测靶点蛋白表达水平。结果：不同剂量的 Axitinib 治疗以剂量依赖的方式显著降低了 A2780、RMG1 和 HeyA 8中磷酸化 EGFR2 的表达，但在 HeyA8 MDR 细胞中没有。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Axitinib (30 mg/kg，0.5% methyl cellulose) 口服给药给携带 A2780、RMG1 或 HeyA8 MDR 肿瘤的 BALB/c nude 小鼠，每天两次，持续 35-40 天。结果：在 A2780 和 RMG1 模型中，Axitinib 治疗组的肿瘤重量与对照组相比显著降低了 50%，但在 HeyA8 MDR 模型中差异不显著。[2]
存储条件	store at low temperature,keep away from moisture,keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 9.7 mg/mL (25 mM)
关键字	inhibit \| Platelet-derived growth factor receptor \| Inhibitor \| Axitinib \| Vascular endothelial growth factor receptor \| AG013736 \| VEGFR \| AG 013736 \| PDGFR
相关产品	Imatinib \| Gilteritinib \| Ribociclib \| Sorafenib tosylate \| Lenvatinib mesylate \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| Pexidartinib \| Regorafenib monohydrate \| Taxifolin
相关库	抑制剂库 \| 经典已知活性库 \| FDA 上市药物库 \| 膜蛋白靶向化合物库 \| FDA 上市激酶抑制剂库 \| 酪氨酸激酶分子库 \| 抗癌药物库

阿昔替尼|||阿西替尼|||AG-013736|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子