Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶 (RTK) 抑制剂,可以抑制 VEGFR2 和 PDGFRβ (IC50=80/2 nM)。Sunitinib 具有抗肿瘤活性,可以用于治疗肾癌和胃肠道肿瘤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | ¥ 543 | 现货 | ||
200 mg | ¥ 798 | 现货 | ||
500 mg | ¥ 1,255 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 218 | 现货 |
产品描述 | Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors. |
靶点活性 | PDGFRβ:2 nM, VEGFR2:80 nM |
体外活性 |
方法:FLT3-ITD 细胞系 MV4;11 和 FLT3-WT 细胞系 OC1-AML5 用 Sunitinib (0.001-10 µM) 处理 48 h,使用 Alamar blue assay 检测细胞活力。 结果:Sunitinib 以剂量依赖性方式显著抑制 MV4;11和 OC1-AML5 细胞增殖,IC50 分别为 8 nM 和 14 nM。[1] 方法:胃肠道间质瘤细胞 GIST-T1 用 Sunitinib (10-40 nM) 处理 48 h,使用 Western Blot 检测靶点蛋白表达水平。 结果:Sunitinib 以剂量依赖的方式抑制 c-KIT 的自磷酸化。Sunitinib 可有效阻断 c-KIT 下游效应子 Akt 和 ERK 的磷酸化,但不影响 STAT3 和 STAT5 的磷酸化形式。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Sunitinib (1-40 mg/kg in a citrate-buffered solution (pH 3.5)) 灌胃给药给携带人白血病肿瘤 MV4;11 的 athymic nu/nu 小鼠,每天一次,至肿瘤消退。 结果:Sunitinib 以 4 0和 20mg/kg/d 给药时表现出剂量依赖性疗效,并消退了已建立的大的皮下肿瘤。[1] 方法:为检测体内抗肿瘤活性,将 Sunitinib (40-80 mg/kg in CMC) 灌胃给药给注射乳腺癌细胞 MDA-MB-435/HAL 的 athymic nu/nu 小鼠,每天一次,持续二十一天。 结果:Sunitinib 治疗荷瘤小鼠后,血清 PYD 水平显著降低,证实了骨溶解的体内抑制作用。使用 BLI,Sunitinib 以 40mg/kg/天治疗 21 天显示出 64% 的骨肿瘤生长抑制作用,以 80mg/kg/天显示出 89% 的抑制作用。[3] |
激酶实验 | Biochemical Tyrosine Kinase Assays: IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST.The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate. |
细胞实验 | Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3. (Only for Reference) |
别名 | 苏尼替尼, 舒尼替尼, SU 11248 |
分子量 | 398.47 |
分子式 | C22H27FN4O2 |
CAS No. | 557795-19-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (62.74 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5096 mL | 12.548 mL | 25.096 mL | 62.74 mL |
5 mM | 0.5019 mL | 2.5096 mL | 5.0192 mL | 12.548 mL | |
10 mM | 0.251 mL | 1.2548 mL | 2.5096 mL | 6.274 mL | |
20 mM | 0.1255 mL | 0.6274 mL | 1.2548 mL | 3.137 mL | |
50 mM | 0.0502 mL | 0.251 mL | 0.5019 mL | 1.2548 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Sunitinib 557795-19-4 Angiogenesis Apoptosis Autophagy Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors Mitophagy VEGFR FLT IRE1 PDGFR c-Kit Inositol requiring enzyme 1 Platelet-derived growth factor receptor Vascular endothelial growth factor receptor inhibit Inhibitor 苏尼替尼 舒尼替尼 SU11248 SU-11248 SU 11248 Mitochondrial Autophagy inhibitor