瑞格非尼一水合物|T1792L|TargetMol

Regorafenib monohydrate
1019206-88-2

￥192 5mg 起订

￥297 10mg 起订

￥515 25mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 瑞格非尼一水合物

英文名称：: Regorafenib monohydrate

CAS号：: 1019206-88-2

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：: 99.69%

产品类别：: 抑制剂

货号：: T1792L

Product Introduction

Bioactivity

名称	Regorafenib monohydrate
描述	Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
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	Regorafenib有效抑制了包括血管生成和基质RTKs VEGFR1-3、TIE2、FGFR1及PDGFR-b在内的一系列特定激酶（IC50s：4-311 nM），以及癌变RTKs KIT和RET，还有细胞内信号激酶c-RAF/RAF-1、BRAF及其V600E变异体（IC50s：1.5-28 nM）。此外，Regorafenib在NIH-3T3/VEGFR2细胞中强效抑制VEGFR2自磷酸化（IC50：3 nM）。在HAoSMCs中，Regorafenib 经PDGF-BB刺激后抑制PDGFR-b自磷酸化（IC50：90 nM）[1]。Regorafenib导致Hep3B细胞生长浓度依赖性下降（IC50：5 μM）。PLC/PRF/5细胞对Regorafenib的响应与Hep3B细胞相似，但HepG2细胞更敏感（IC50：1 μM）[2]。
体内活性	给带瘤大鼠单次口服regorafenib 10 mg/kg可显著降低肿瘤灌注和对比剂的渗出。regorafenib处理后10小时，归一化的IAUC360显著降低，并持续至2天，与对照组相比。regorafenib通过口服每日一次（qd）的剂量依赖方式抑制了在多种异种移植模型中的肿瘤生长，包括来自CRC（Colo-205）、BC（MDA-MB-231）和RCC（786-O）肿瘤的模型。regorafenib (10–100 mg/kg)有效抑制了Colo-205异种移植体的生长，在10 mg/kg剂量时，第14天的肿瘤生长抑制（TGI）达到约75%[1]。在小鼠异种移植模型中，口服regorafenib、M-2和M-5与对照相比显著抑制了肿瘤的生长。小鼠反复口服regorafenib 10 mg/kg/day后，M-2和M-5在小鼠体内的总峰值血浆化合物浓度和暴露程度与人类相当[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 : 20 mg/mL (39.93 mM)
关键字	tumor \| Colo-205 \| HUVECs \| PDGFR \| NIH-3T3 \| Regorafenib monohydrate \| inhibit \| Raf kinases \| antiangiogenic \| Regorafenib Monohydrate \| Hep3B cell \| Autophagy \| HAoSMCs \| Vascular endothelial growth factor receptor \| Inhibitor \| Antitumorigenic \| 786-O \| Regorafenib \| Raf \| Platelet-derived growth factor receptor \| VEGFR \| RET \| BAY 73-4506
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瑞格非尼一水合物|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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