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SorafenibRaf激酶和酪氨酸激酶抑制剂

Sorafenib

产品编号:A3009
ApexBio 的所有产品仅用作科研,我们不为任何个人用途提供产品和服务
规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥500.00 现货
20mg ¥660.00 现货
50mg ¥780.00 现货
200mg ¥1,630.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. 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
2. 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

质量控制

化学结构

Sorafenib

相关生物数据

Sorafenib
Sorafenib monotherapy on inhibition of LCSC, Huh7, and PLC cells (MTT assay).

相关生物数据

Sorafenib

相关生物数据

Sorafenib

相关生物数据

Sorafenib

Sorafenib Dilution Calculator

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化学性质

CAS号 284461-73-0 SDF Download SDF
别名 BAY-43-9006,Sorafenib,Nexavar,sorafenibum
化学名 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
SMILES CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
分子式 C21H16ClF3N4O3 分子量 464.82
溶解度 ≥23.25mg/mL in DMSO 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

生物活性

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    

实验操作

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.

研究更新

1. PKI-587 and sorafenib alone and in combination on inhibition of liver cancer stem cell proliferation. J Surg Res. 2013 Nov;185(1):225-30. doi: 10.1016/j.jss.2013.05.016. Epub 2013 May 25.
Abstract
The anti-proliferation induced by dual inhibition of PI3 K/Akt/mTOR signaling pathways and Ras/Raf/mitogen-activated protein kinase, which are associated with HCC proliferation, has been evaluated in non-liver cancer stem cell lines and LCSC lines respectively.
2. Alternative formulations of sorafenib for use in children. Pediatr Blood Cancer. 2013 Oct;60(10):1642-6. doi: 10.1002/pbc.24619. Epub 2013 Jun 20.
Abstract
Since the 200 mg tablet of sorafenib, a multikinase inhibitor with antiangiogenic and antitumor activity, is not suitable for children, extemporaneously prepared smaller-dosage of sorafenib has been investigated for stability and pharmacokinetic profile in children.
3. Sorafenib prolongs liver regeneration after hepatic resection in rats. J Surg Res. 2013 Oct;184(2):847-54. doi: 10.1016/j.jss.2013.04.062. Epub 2013 May 18.
Abstract
Sorafenib is a multikinase inhibitor that exhibits antiangiogenic and antiproliferative activity and targets signaling pathways involved in liver regeneration.
4. Iron-dependent cell death of hepatocellular carcinoma cells exposed to sorafenib. Int J Cancer. 2013 Oct 1;133(7):1732-42. doi: 10.1002/ijc.28159. Epub 2013 Apr 8.
Abstract
Sorafenib is a multikinase inhibitor that exerts cytotoxic effects on HCC cells through inducing ferroptosis, a iron-dependent and oxidative stress-associated cell death.
5. Hand-foot skin reaction is associated with the clinical outcome in patients with metastatic renal cell carcinoma treated with sorafenib. Jpn J Clin Oncol. 2013 Oct;43(10):1023-9. doi: 10.1093/jjco/hyt110. Epub 2013 Aug 15.
Abstract
The association between the Hand-Foot skin reaction and the clinical outcome in metastatic renal cell carcinoma patients treated with sorafenib were retrospectively examined.

产品描述

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