Sorafenib
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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. 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
- 2. 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
- 3. 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
- 4. 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
- 5. 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
- 6. 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
- 7. 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
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