Sorafenib
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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.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
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是一种可口服的多激酶抑制剂,作用于Raf激酶和几种受体酪氨酸激酶,包括血管内皮生长因子受体2(VEGFR2)、血小板衍生生长因子受体(PDGFR)、FLT3、Ret和c-Kit。Sorafenib通过抗增殖、抗血管生成和/或促凋亡效应,从而抑制肿瘤生长,破坏肿瘤微血管。在体外,sorafenib阻断Raf激酶信号,抑制肿瘤细胞增殖,诱导细胞凋亡。此外,sorafenib具有强烈的抗肿瘤功效。
参考文献:
1. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. L Liu, Y Cao, C Chen, X Zhang, A McNabola, D Wilkie Cancer research, 2006
2. Phase II study ofsorafenibin patients with advanced hepatocellular carcinoma. GK Abou-Alfa, L Schwartz, S Ricci. Journal of clinical Oncology. 2006
- 1. Yi-Jen Liao, et al. "Long-term di-(2-ethylhexyl) phthalate exposure reduces sorafenib treatment efficacy by enhancing mesenchymal transition in hepatocellular carcinoma." Ecotoxicol Environ Saf. 2024 Mar 15:273:116161. PMID: 38430581
- 2. Linzhuo Huang, Rui Xu, et al. "Repolarization of macrophages to improve sorafenib sensitivity for combination cancer therapy." Acta Biomater. 2023 May:162:98-109. PMID: 36931417
- 3. Seoyul Lee, Wookyeom Yang, et al. "Inhibition of MEK-ERK pathway enhances oncolytic vaccinia virus replication in doxorubicin-resistant ovarian cancer." Mol Ther Oncolytics. 2022 Apr 18;25:211-224. PMID: 35592390
- 4. CHONG ZHANG, LIN‑WEN WU, et al. "DYRK1A suppression attenuates HIF‑1α accumulation and enhances the anti‑liver cancer effects of regorafenib and sorafenib under hypoxic conditions." Int J Oncol. 2022 Apr;60(4):45. PMID: 35244188
- 5. Zhou Yu, Jiaying Du, et al. "LT-171-861, a novel FLT3 inhibitor, shows excellent preclinical efficacy for the treatment of FLT3 mutant acute myeloid leukemia." Theranostics. 2021 Jan 1;11(1):93-106. PMID: 33391463
- 6. Qi Wang, Yaxun Guo, et al. "RNA binding protein DAZAP1 promotes HCC progression and regulates ferroptosis by interacting with SLC7A11 mRNA." Exp Cell Res. 2021 Feb 1;399(1):112453. PMID: 33358859
- 7. Bai J, Liu Z, et al. "Mitochondrial metabolic study guided by proteomics analysis in hepatocellular carcinoma cells surviving long-term incubation with the highest dose of sorafenib." Aging (Albany NY), 11 (24), 12452-12475 2019 Dec 26. PMID: 31881007
- 8. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID: 30038713
- 9. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID: 29249695
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 464.82 |
Cas No. | 284461-73-0 |
Formula | C21H16ClF3N4O3 |
Synonyms | BAY-43-9006,Sorafenib,Nexavar,sorafenibum |
Solubility | ≥23.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | 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 |
PLC/PRF/5和HepG2细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃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℃可放置数月 |
反应条件 |
IC50: PLC/PRF/5细胞的IC50值为6.3 μM,HepG2细胞的IC50值为4.5 μM,72 hours |
实验结果 |
通过CellTiter-Glo测定法测量sorafenib对细胞增殖的影响,Sorafenib以剂量依赖性的方式抑制细胞增殖,抑制PLC/PRF/5的IC50值为6.3 μmol/L,抑制HepG2细胞的IC50值为4.5 μmol/L |
动物实验[1]: | |
动物模型 |
注射PLC/PRF/5细胞的雌性CB17SCID小鼠 |
剂量 |
口服;10、30和100 mg/kg;每天一次,持续16或21天 |
实验结果 |
在皮下移植PLC/PRF/5肿瘤异种移植物的SCID小鼠中,Sorafenibtosylate以剂量依赖性的方式抑制肿瘤生长。10和30 mg/kg的剂量水平产生显著的剂量依赖性抑制,TGI分别为49%和78%。100 mg/kg剂量水平的sorafenibtosylate在50%的小鼠中产生持久的部分肿瘤消退作用。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Liu L, Cao Y, Chen C, et al. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. Cancer research, 2006, 66(24): 11851-11858. |
描述 | Sorafenib是一种多激酶抑制剂,作用于Raf-1、B-Raf和VEGFR-2,IC50值分别为6 nM、22 nM和90 nM。 | |||||
靶点 | 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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