舒尼替尼|T0374L

Sunitinib
557795-19-4

￥543 100mg 起订

￥1255 500mg 起订

￥798 200mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 舒尼替尼

英文名称：: Sunitinib

CAS号：: 557795-19-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.67%

产品类别：: 抑制剂

货号：: T0374L

Product Introduction

Bioactivity

名称	Sunitinib
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.
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)
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.
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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 25 mg/mL (62.74 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.25 mg/mL (3.14 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	Sunitinib \| PDGFR \| Inositol requiring enzyme 1 \| IRE1 \| Platelet-derived growth factor receptor \| Autophagy \| Mitophagy \| Vascular endothelial growth factor receptor \| inhibit \| Inhibitor \| SU11248 \| VEGFR \| SU-11248 \| Apoptosis \| Mitochondrial Autophagy
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相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| EMA 上市药物库 \| 激酶抑制剂库 \| FDA 上市药物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 抗癌药物库

苏尼替尼|||舒尼替尼|||SU 11248|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
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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