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Regorafenib monohydrate

产品编号 T1792LCas号 1019206-88-2
别名 瑞格非尼一水合物

Regorafenib monohydrate 是一种新型口服多激酶抑制剂,对VEGFR1/2/3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。

Regorafenib monohydrate

Regorafenib monohydrate

纯度: 99.69%
产品编号 T1792L 别名 瑞格非尼一水合物Cas号 1019206-88-2

Regorafenib monohydrate 是一种新型口服多激酶抑制剂,对VEGFR1/2/3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。

规格价格库存数量
5 mg¥ 192现货
10 mg¥ 297现货
25 mg¥ 515现货
50 mg¥ 787现货
100 mg¥ 1,230现货
200 mg¥ 1,790现货
500 mg¥ 2,960现货
1 mL x 10 mM (in DMSO)¥ 397现货
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"Regorafenib monohydrate"的相关化合物库

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纯度:99.69%
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产品介绍

生物活性
产品描述
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.
靶点活性
VEGFR1:13 nM, c-Kit:7 nM, RET kinase:1.5 nM
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]。
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.
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].
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].
别名瑞格非尼一水合物
化学信息
分子量500.83
分子式C21H17ClF4N4O4
CAS No.1019206-88-2
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 20 mg/mL (39.93 mM)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.9967 mL9.9834 mL19.9669 mL99.8343 mL
5 mM0.3993 mL1.9967 mL3.9934 mL19.9669 mL
10 mM0.1997 mL0.9983 mL1.9967 mL9.9834 mL
20 mM0.0998 mL0.4992 mL0.9983 mL4.9917 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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

剂量转换

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