资料发布时间:2018-10-30 14:50:00 最后更新时间: 2021-06-09 15:17:08
【药品简介】 阿昔替尼能抑制酪氨酸激酶受体包括血管内皮生长因子受体(VEGFR)-1,VEGFR-2和VEGFR-3。阿西替尼通过同这些受体结合,从而抑制肿瘤血管生成,减缓肿瘤生长和病情进展。
【适应症状】 阿昔替尼,本品为抗肿瘤药,临床上主要用于既往接受过一种酪氨酸激酶抑制剂或细胞因子治疗失败的进展期肾细胞癌(RCC)的成人患者。
【 药品别名 】 阿昔替尼 Axitinib Inlyta
印度阿昔替尼(阿昔替尼 Axitinib Inlyta)价格,正品图片,治疗肾癌药物, 购买阿昔替尼请到印度药房官方网站进行购买 【印度药房大全目录】
【 市场参考价格 】 ¥1180.00~1580.00
播放/暂停
产品描述 |
Axitinib is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively. |
靶点活性 |
PDGFRβ,1.6 nM VEGFR1/FLT1,0.1 nM VEGFR2/Flk1,0.18 nM VEGFR2/KDR,0.2 nM VEGFR3,0.1-0.3 nM Kit,1.7 nM |
实验溶液 |
0.5% CMC: 30 mg/mL |
体外活性 |
In transfected or endogenous RTK-expressing cells, axitinib potently blocked growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 (IC50s: 0.2 and 0.1 to 0.3 nmol/L, respectively). Cellular activity against VEGFR-1 was 1.2 nmol/L. Axitinib rapidly and dose-dependently reduced the phosphorylation of Akt, endothelial nitric oxide synthase (eNOS), and extracellular signal-regulated kinase 1/2 (ERK1/2), key downstream signaling molecules of VEGF [1]. Axitinib reduced cell viability in a dose-dependent manner with IC50 doses of >10,000, 849 and 274 nmol/l for IGR-N91, IGR-NB8, and SH-SY5Y, respectively. the sensitivity to axitinib of neuroblastoma cell lines appeared to be in a similar range as non-VEGF stimulated HUVEC (IC50: 573 nmol/l) [2]. |
体内活性 |
Acute axitinib treatment rapidly and significantly reduced retinal vascular VEGFR-2 phosphorylation. One hour after the second dose, retinal VEGFR-2 phosphorylation was reduced by 80% to 90% compared with that of the control tissues. Six and 24 to 32 h post-dose, the phospho-VEGFR-2 levels returned to 50% and 100% of the control, respectively. The EC50 value for the inhibition of VEGFR-2 phosphorylation was 0.49 nmol/L [1]. Mice were next treated for a period of 2 weeks with either fractionated radiation (5 × 2 Gy/wk) or AG-013736 (25 mg/kg/d) and 1 to 3 weeks for the combination. Tumor volume at the end of 2 weeks was significantly reduced for either single or combination treatments. Percentage increases in tumor volume were similar between radiotherapy (40 ± 9.8%) and AG-013736 (48 ± 9.2%), and the combination was markedly reduced versus controls (12 ± 5.7% versus 77 ± 11%) [3]. |
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]. |
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]. 细胞系: HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells |
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]. 动物模型:BT474 breast cancer cells are implanted subcutaneously into Immune-deficient femice (Nu/nu; age 8-12 weeks). |
化学信息
分子量 |
386.47 |
分子式 |
C22H18N4OS |
CAS |
319460-85-0 |
溶解度 |
DMSO: 9.7 mg/mL (25 mM) ( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 2.588 ml | 12.938 ml | 25.875 ml |
5 mM | 0.518 ml | 2.588 ml | 5.175 ml |
10 mM | 0.259 ml | 1.294 ml | 2.588 ml |
50 mM | 0.052 ml | 0.259 ml | 0.518 ml |
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