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Sunitinib

Sunitinib

产品编号 T0374L   CAS 557795-19-4
别名: 苏尼替尼, 舒尼替尼, SU 11248

Sunitinib (SU 11248) 是一种 ATP 竞争性抑制剂,通过抑制自身磷酸化和 RNase 激活来有效抑制 Ire1α的磷酸化。它还是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2和 PDGFRβ的IC50分别为 80 nM 和 2 nM

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Sunitinib Chemical Structure
Sunitinib, CAS 557795-19-4
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
其他形式的 Sunitinib:
产品目录号及名称: Sunitinib (T0374L)
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选择批次  
纯度: 99.67%
纯度: 98.62%
纯度: 98.38%
纯度: 98.22%
纯度: 98%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Sunitinib (SU 11248), a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
靶点活性 PDGFRβ:2 nM, VEGFR2:80 nM
体外活性 在FLT3-ITD骨髓移植模型中,Sunitinib(每天20 mg/kg)对皮下MV4;11 (FLT3-ITD)异种移植物的生长具有明显抑制作用,并延长生存.与实质性,选择性抑制VEGFR2或PDGFR在体内的磷酸化和信号传导一致,Sunitinib(每天20-80 mg/kg)对各种肿瘤异种移植模型,包括HT-29,Colo205,A431,SF763T,C6,H-460,A375或MDA-MB-435表现出广泛有效的剂量依赖性抗肿瘤活性.Sunitinib(每天80 mg/kg)给药21天,8只小鼠中有6只的肿瘤完全消退,且在治疗结束后的110天的观察期内肿瘤没有再生.尽管不能完全恢复到第一轮治疗的情况,但在第二轮使用Sunitinib治疗仍然能够有效抗肿瘤.Sunitinib治疗可使肿瘤MVD明显下降,如在SF763T神经胶质瘤中可减少~40%.尽管肿瘤没有减小,SU11248治疗还是能够完全抑制表达荧光素酶的PC-3M异种移植的肿瘤生长.
体内活性 Sunitinib是PDGFRβ(Ki:8 nM)和 VEGFR2 (Flk1)(Ki:9 nM)有效的ATP竞争性抑制剂。与FGFR-1,EGFR,Cdk2,Met,IGFR-1,Abl,和src相比,Sunitinib作用于VEGFR2和PDGFR的选择性要高出10倍。在血清饥饿的表达PDGFRβ或VEGFR2的NIH-3T3细胞中,Sunitinib抑制VEGF依赖性VEGFR2磷酸化和PDGF依赖性PDGFRβ磷酸化,IC50均为10 nM。Sunitinib抑制野生型FLT3-ITD,FLT3-Asp835和FLT3磷酸化,IC50分别为50 nM,30 nM和250 nM。Sunitinib抑制OC1-AML5和MV4;11 细胞的增殖,IC50分别为14 nM和8 nM,并以剂量依赖的方式诱导细胞凋亡。Sunitinib能够有效抑制FLT-3和Kit。对于过表达PDGFRα或PDGFRβ的NIH-3T3细胞,Sunitinib抑制VEGF对其诱导的增殖,IC50 分别为69 nM和39 nM。
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 25 mg/mL (62.74 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Sun L, et al. J Med Chem, 2003, 46(7), 1116-1119. 2. Mendel DB, et al. Clin Cancer Res, 2003, 9(1), 327-337. 3. O'Farrell AM, et al. Blood, 2003, 101(9), 3597-3605. 4. Abrams TJ, et al. Mol Cancer Ther, 2003, 2(10), 1011-1021. 5. Yee KW, et al. Blood, 2004, 104(13), 4202-4209.

文献引用

1. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22. 2. Oeller M, Jaksch-Bogensperger H, Templin M, et al.Transcription Factors STAT3 and MYC Are Key Players of Human Platelet Lysate-Induced Cell Proliferation.International Journal of Molecular Sciences.2022, 23(24): 15782. 3. Xue K H, Jiang Y F, Bai J Y, et al.Melatonin suppresses Akt/mTOR/S6K activity, induces cell apoptosis, and synergistically inhibits cell growth with sunitinib in renal carcinoma cells via reversing Warburg effect.Redox Report.2023, 28(1): 2251234. 4. Liu T, Yue X, Chen X, et al.Nilotinib in combination with sunitinib renders MCL-1 for degradation and activates autophagy that overcomes sunitinib resistance in renal cell carcinoma.Cellular Oncology.2024: 1-18.
AG 1295 PD-161570 Agerafenib Methylnissolin Linifanib PD168393 SU14813 Ponatinib

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌药物库 抗癌临床化合物库 铜死亡化合物库 内质网应激化合物库 口服活性化合物库 细胞凋亡化合物库 细胞周期化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

Sunitinib 557795-19-4 Angiogenesis Apoptosis Autophagy Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors FLT Mitophagy VEGFR 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

 

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