Sorafenib Tosylate
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Sorafenib tosylate(甲苯磺酸索拉非尼),也称为Nexavar(多吉美),是一种小分子抗癌药物[1],也是一种新型可口服的Raf激酶和血管内皮生长因子受体(VEGFR)抑制剂,抑制肿瘤细胞的增殖和肿瘤血管生成[2]。在HepG2细胞(1×106)中,sorafenib tosylate的IC50值为2.09 μg/ml[3]。
Raf是一种有丝分裂原刺激蛋白激酶,作为信号级联反应的成分,刺激有丝分裂原活化蛋白激酶[4]。血管内皮生长因子(VEGF)是血管内皮细胞高特异性的有丝分裂原[5]。
在MV4-11(FLT3-ITD)细胞中,nexavar以剂量依赖的方式有效抑制细胞增殖,IC50值为0.88 nM。在MV4-11细胞中,sorafenib tosylate在100 nM浓度时诱导43.6±5.2%的细胞凋亡,而在EOL-1细胞中,在浓度低至10 nM时可诱导89.29±1.8%的细胞凋亡[6]。
在注射105个MDA-MB-231细胞的6周龄裸大鼠中,与对照组相比,sorafenib tosylate单独给药后,在第45天和第55天观察到溶骨性病变体积的显著减少,在第55天观察到软组织成分的显著减少(p < 0.05)。与对照相比,sorafenib tosylate治疗使得骨转移的振幅A显著下降,从第35天一直持续到第55天(振幅A:p<0.01;维持,第35天和第55天,p<0.01;第45天p<0.05)[7]。
参考文献:
[1]. Chetan Lathia, John Lettieri, Frank Cihon, et al. Lack of effect of ketoconazole-mediated CYP3A inhibition on sorafenib clinical pharmacokinetics. Cancer Chemother Pharmacol, 2006, 57: 685-692.
[2]. M. J. Gnoth, S. Sandmann, K. Engel, et al. In Vitro to In Vivo Comparison of the Substrate Characteristics of Sorafenib Tosylate toward P-Glycoprotein. Drug Metabolism & Disposition, 2010, 38: 1341–1346.
[3]. Sayantan Dey, Subhadeep Roy, Nilanjana Deb, et al. Anti-carcinogenic Activity of Ruellia Tuberosa L. (Acanthaceae) Leaf Extract on Hepatoma Cell Line & Increased Superoxide Dismutase Activity on Macrophage Cell Lysate. Int J Pharm Pharm Sci, 2010, 5(Suppl 3): 854-861.
[4]. Markus Wartmann and Roger J. Davis. The Native Structure of the Activated Raf Protein Kinase Is a Membrane-bound Multi-subunit Complex. The Journal of Biological Chemistry, 1994, 269(9): 6695-6701.
[5]. Gera Neufeld, Tzafra Cohen, Stela Gengrinovitch, et al. Vascular endothelial growth factor (VEGF) and its receptors. The FASEB Journal, 1999, 13: 9-22.
[6]. D Auclair, D Miller, V Yatsula, et al. Antitumor activity of sorafenib in FLT3-driven leukemic cells. Leukemia, 2007, 21:439-445.
[7]. Maximilian Merz, Dorde Komljenovic, Stefan Zwick, et al. Sorafenib tosylate and paclitaxel induce anti-angiogenic, anti-tumour and anti-resorptive effects in experimental breast cancer bone metastases. European Journal of Cancer, 2011, 47:277-286.
- 1. Liao YJ, Hsu SM, et al. "Treatment with a New Barbituric Acid Derivative Exerts Antiproliferative and Antimigratory Effects against Sorafenib Resistance in Hepatocellular Carcinoma." Molecules. 2020;25(12):E2856. PMID:32575795
- 2. Suk FM, Liu CL, et al. "Treatment with a new benzimidazole derivative bearing a pyrrolidine side chain overcomes sorafenib resistance in hepatocellular carcinoma." Sci Rep. 2019 Nov 21;9(1):17259. PMID:31754201
- 3. Ming-Hua Hsu, Shih-Ming Hsu, et al. "Treatment with low-dose sorafenib in combination with a novel benzimidazole derivative bearing a pyrolidine side chain provides synergistic anti-proliferative effects against human liver cancer." RSC Adv., 2017, 7, 16253-16263.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 637.03 |
Cas No. | 475207-59-1 |
Formula | C21H16ClF3N4O3·C7H8O3S |
Solubility | ≥31.85 mg/mL in DMSO; insoluble in H2O; ≥4.15 mg/mL in EtOH with ultrasonic |
Chemical Name | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide;4-methylbenzenesulfonic acid |
SDF | Download SDF |
Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)O.CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
MV4-11细胞和EOL-1细胞 |
制备方法 |
在DMSO中的溶解度大于31.9 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
100 pM ~ 10 μM;MV4-11细胞:72小时,EOL-1细胞:24小时 |
实验结果 |
在浓度为100 nM时,Sorafenib 促进43.6 ± 5.2%细胞经历细胞凋亡。在EOL-1细胞中,即使浓度低至10 nM,Sorafenib也能促进89.29 ± 1.8%细胞经历细胞凋亡。对经过Sorafenib治疗的MV4-11细胞的细胞周期进行分析,结果显示,Sorafenib呈剂量依赖性地诱导细胞周期停滞,处于G0/G1期的细胞百分比从52.7 ± 0.9%(对照组)增至66.8 ± 1.5%(100 nM Sorafenib组)。 |
动物实验 [1]: | |
动物模型 |
携带FLT3-ITD肿瘤的无胸腺小鼠 |
给药剂量 |
0.3、1.0、3或10 mg/kg;口服给药 |
实验结果 |
在携带FLT3-ITD肿瘤的无胸腺小鼠中,Sorafenib显示出剂量依赖性的抗肿瘤活性。在3 mg/kg和10 mg/kg的剂量下,10只小鼠中的6和9只分别显示完全的反应。MV4-11肿瘤的蛋白印迹实验结果显示,在第2次给药3小时后,STAT5磷酸化被完全抑制。同时,磷酸化组蛋白H3水平也显著降低。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. D Auclair, D Miller, V Yatsula, et al. Antitumor activity of sorafenib in FLT3-driven leukemic cells. Leukemia, 2007, 21:439-445. |
Description | Sorafenib Tosylate(Bay 43-9006)是一种多靶点激酶抑制剂,作用于Raf-1、B-Raf和VEGFR-2,IC50值分别为6 nM、22 nM和90 nM。 | |||||
靶点 | Raf-1 | B-Raf | VEGFR2 | PDGFRβ | ||
IC50 | 6 nM | 22 nM | 90 nM | 57 nM |
质量控制和MSDS
- 批次:
化学结构
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