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Sorafenib.

(Synonyms: 索拉非尼; Bay 43-9006)

目录号: PC16011 纯度: ≥98%

Raf激酶和酪氨酸激酶抑制剂,Sorafenib (Bay 43-9006) 是有效的多激酶抑制剂，抑制Raf-1，B-Raf 和 VEGFR-3 的 IC50 分别为6 nM，20 nM，22 nM。

CAS No. :284461-73-0

商品编号	规格	价格	会员价
PC16011-5mg	5mg	¥148.00	请登录
PC16011-10mg	10mg	¥193.00	请登录
PC16011-25mg	25mg	¥313.00	请登录
PC16011-50mg	50mg	¥418.00	请登录
PC16011-100mg	100mg	¥651.00	请登录
PC16011-500mg	500mg	¥989.00	请登录
PC16011-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥267.00	请登录

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中文名称

Sorafenib.

中文别名

索拉非尼;4-{4-[3-(4-氯-3-三氟甲基苯基)酰脲]苯氧基}吡啶-2-甲酰胺;对甲苯磺酸索拉非尼;索拉菲尼;索+E51拉尼;索拉非尼碱;索拉替尼;索拉菲尼碱;O-(2-氨乙基)-O`-[2-(BOC-氨乙基]五缩六乙二醇;Sorafenib tosylate 索拉非尼;Sorafenib tosylate 索拉非尼标准品;甲磺酸索拉非尼;硫酸颠茄碱;索拉非尼、索拉非尼碱、索拉菲尼;索拉非尼-D4;索拉非尼标准品;索拉非尼对甲苯磺酸索拉非尼;索拉非尼杂质;索拉非尼杂质库存;索拉非尼杂质及标准品;索拉非尼中间体;索拉菲尼标准品及杂质;索拉菲尼杂质;索拉菲尼杂质及标准品;索拉菲尼中间体2;托西酸索拉非尼;Raf抑制剂;舒拉非尼;索拉菲尼单体;索拉替尼

英文名称

Sorafenib

英文别名

Sorafenib tosylate;sorafenib;SORAFENIB-D3;SORAFENIB TOLSYLATE;RAF1 KINASE INHIBITOR II;N-(4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)-((4-(2-(N-METHYL-CARBAMOYL)(4-PYRIDYLOXY))PHENYL)AMINO)CARBOXAMIDE;4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-n-methyl-pyridine-2-carboxamide;BAY 43-9006;SORAFENIB MESYLATE;BAY-43-9006;Sorafenib (BAY 43-9006);Sorafenib base;Sorafenib Free Base;Epirubicin HCl; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide;BAY-43-900;Forafenib;Nexavar;4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide;N-(4-Chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea;4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide;4-(4-((((4-Chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy;4-(4-((((4-Chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl-2-pyridinecarboxamide;4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy

Cas No.

284461-73-0

分子式

C₂₁H₁₆ClF₃N₄O₃

分子量

464.83

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

Raf激酶和酪氨酸激酶抑制剂,Sorafenib (Bay 43-9006) 是有效的多激酶抑制剂，抑制Raf-1，B-Raf 和 VEGFR-3 的 IC50 分别为6 nM，20 nM，22 nM。

生物活性

Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC₅₀s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC₅₀s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.

性状

Solid

IC50 & Target[1][2]

VEGFR3

20 nM (IC₅₀)

Braf

22 nM (IC₅₀)

Raf-1

6 nM (IC₅₀)

VEGFR2

90 nM (IC₅₀)

PDGFRβ

57 nM (IC₅₀)

Braf

38 nM (IC₅₀)

c-Kit

68 nM (IC₅₀)

Flt3

58 nM (IC₅₀)

体外研究(In Vitro)

Sorafenib (BAY 43-9006) also inhibits BRAF (IC₅₀=22 nM), BRAF (IC₅₀=38 nM), VEGFR-2 (IC₅₀=90 nM), VEGFR-3 (IC₅₀=20 nM), PDGFR-β (IC₅₀=57 nM), c-KIT (IC₅₀=68 nM), and Flt3 (IC₅₀=58 nM) in biochemical assays. In MDA-MB-231 breast cancer cells, Sorafenib completely blocks activation of the MAPK pathway. Cells are preincubated with Sorafenib (0.01 to 3 μM), and dose-dependent inhibition of basal MEK 1/2 and ERK 1/2 phosphorylation (IC₅₀, 40 and 100 nM, respectively).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Sorafenib demonstrates broad oral antitumor efficacy in panel of human tumor xenograft models. Sorafenib is given orally at 7.5 to 60 mg/kg. There is no lethality and no increase in weight loss in any treated group relative to the corresponding control group. Daily oral administration of Sorafenib (30 to 60 mg/kg) produces complete tumor stasis during treatment in five of the six models. The survival rate is 73.3 % in Diethyl nitrosamine (DENA) group and 83.3 % in Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows significant decrease (p<0.05) in liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [Information]

[2]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. [Information]

[3]. Jin W, et al. Long non-coding RNA TUC338 is functionally involved in sorafenib-sensitized hepatocarcinoma cells by targeting RASAL1. Oncol Rep. 2017 Jan;37(1):273-280. [Information]

[4]. Li M, et al. Activation of an AKT/FOXM1/STMN1 pathway drives resistance to tyrosine kinase inhibitors in lung cancer. Br J Cancer. 2017 Aug 29. [Information]

溶解度数据

体外研究:

DMSO : ≥ 45 mg/mL (96.81 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1513 mL	10.7566 mL	21.5132 mL
5 mM	0.4303 mL	2.1513 mL	4.3026 mL
10 mM	0.2151 mL	1.0757 mL	2.1513 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (4.47 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [Information]

[2]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. [Information]

[3]. Jin W, et al. Long non-coding RNA TUC338 is functionally involved in sorafenib-sensitized hepatocarcinoma cells by targeting RASAL1. Oncol Rep. 2017 Jan;37(1):273-280. [Information]

[4]. Li M, et al. Activation of an AKT/FOXM1/STMN1 pathway drives resistance to tyrosine kinase inhibitors in lung cancer. Br J Cancer. 2017 Aug 29. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Sorafenib.

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