瑞戈非尼|T1792|TargetMol

Regorafenib
755037-03-7

￥192 5mg 起订

￥298 10mg 起订

￥515 25mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 瑞戈非尼

英文名称：: Regorafenib

CAS号：: 755037-03-7

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：: 99.95%

产品类别：: 抑制剂

货号：: T1792

Product Introduction

Bioactivity

名称	Regorafenib
描述	Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
细胞实验	Each cell line was seeded at 0.3×10^5 cells/2ml of DMEM containing 10% FBS in 35 mm tissue culture dishes. The cells were incubated for 24 h to allow attachment, and then the medium was replaced by fresh culture medium containing Regorafenib at increasing concentrations (1 μM, 2.5 μM, 5 μM, 7.5 μM and 10 μM). In these experimental conditions, the cells were allowed to grow for 72 or 96 h. Time-course experiments on Hep3B cells were performed with 7.5 μM of Regorafenib at short (15, 60, 180 min.), middle (24, 48, 72 and 96 h) or long times (up to seven days). When the cells were treated for long times the drug was replaced with a fresh one. Each experiment included a control with the equivalent concentration of DMSO (solvent control) as the one used for adding Regorafenib. Each experiment was performed in triplicate and repeated 3 times. Subsequent analyses were performed at specific Regorafenib concentrations and incubation times [2].
激酶实验	In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFR-b (aa561–aa1106), RAF-1 (aa305–aa648) and BRAFV600E (aa409–aa765) kinase domains were performed as previously described. Initial in vitro kinase inhibition profiling was performed at a fixed 1 μM compound concentration under Millipore standard conditions [10 μM adenosine-50'- triphosphate (ATP) concentration]. Inhibitory concentration of 50% (IC50) values were determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition was measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
动物实验	Female athymic NCr nu/nu mice, kept in accordance with Federal guidelines, were subcutaneously inoculated with 5×10^6 Colo-205 or MDAMB-231 cells or implanted with 1 mm^3 786-O tumor fragments. When tumors reached a volume of ~100 mm^3, regorafenib or vehicle control was administered orally qd×21 in the 786-O model, and qd×9 in the Colo-205 and MDA-MB231 models, respectively, at doses of 100, 30, 10, and 3 mg/kg. Paclitaxel was administered intravenously at 10 mg/kg in ethanol/Cremophor ELV/saline (12.5%/12.5%/75%) every 2 days×5. Tumor size (volume) was estimated twice weekly (l×w^2)/2, and the percentage of tumor growth inhibition (TGI) was obtained from terminal tumor weights (1-T/C100). Mice were weighed every other day starting from the first day of treatment. The general health status of the mice was monitored daily [1].
体外活性	方法：人肝癌细胞 Hep3B、PLC/PRF/5 和 HepG2 用 Regorafenib (0-10 μM) 处理 72 h，使用 MTT 方法检测细胞活力。结果：Regorafenib 浓度依赖性降低 Hep3B 细胞活力，IC50 约为 5 μM。PLC/PRF/5 细胞的敏感性与 Hep3B细胞相似。但 HepG2 细胞更敏感，IC50 约为 1 μM。[1] 方法：肿瘤细胞 NIH-3T3/VEGFR2、CHO/TIE2、HAoSMC/PDGFR-β 和 MCF-7/FGFR 用 Regorafenib (10-3000 nM) 处理 1 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Regorafenib 抑制 p-VEGFR2、p-TIE2、p-PDGFR-β 和 p-FGFR。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Regorafenib (3-100 mg/kg) 口服给药给携带肿瘤 Colo-205 或 MDA-MB-231 的 NCr nu/nu 小鼠，每天一次，持续九天。结果：Regorafenib 抑制肿瘤生长。Colo-205 模型中，Regorafenib 在 10 mg/kg 的剂量下，第 14 天的 TGI 达到 75%。MDA-MB-231 模型，Regorafenib 在低至 3 mg/kg 的剂量下是高效的，导致 81% 的显著TGI。[2] 方法：为检测体内抗肿瘤活性，将 Regorafenib (3-10 mg/kg) 口服给药给携带肿瘤 HT-29 或 MDA-MB-231 的 NMRI nu/nu 小鼠，每天一次，持续二十七天。结果：Regorafenib 剂量依赖性抑制 HT-29 和 MDA-MB-231 肿瘤生长。[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 : 60 mg/mL (124.27 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 9 mg/mL (18.64 mM), Suspension. 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. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	HUVECs \| Autophagy \| Vascular endothelial growth factor receptor \| Colo-205 \| FGFR \| SCFR \| RET \| NIH-3T3 \| antiangiogenic \| Antitumorigenic \| PDGFR \| inhibit \| c-Kit \| HAoSMCs \| Platelet-derived growth factor receptor \| tumor \| Regorafenib \| Inhibitor \| Hep3B cell \| CD117 \| Raf kinases \| Fibroblast growth factor receptor \| VEGFR \| Raf \| 786-O
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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 \| 已知活性化合物库 \| 激酶抑制剂库 \| 药物功能重定位化合物库 \| FDA 上市激酶抑制剂库 \| 酪氨酸激酶分子库 \| 抗癌临床化合物库 \| 抗癌药物库

瑞格非尼|||瑞戈非尼|||Fluoro-Sorafenib|||BAY 73-4506|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

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