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索拉非尼

高效多激酶抑制剂

规格或纯度: ≥99%

CAS编号: 284461-73-0
分子式: C₂₁H₁₆ClF₃N₄O₃
分子量: 464.83
PubChem编号: 216239

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货号 (SKU)	包装规格	是否现货	价格	数量
S125098-250mg	250mg	现货
S125098-1g	1g	现货
S125098-5g	5g	现货
S125098-25g	25g	现货
S125098-100g	100g	现货

查看相关系列

B-Raf proto-oncogene，serine/threonine kinase Inhibitor cyclin dependent kinase 19 Inhibitor cyclin dependent kinase 8 Inhibitor discoidin domain receptor tyrosine kinase 2 Inhibitor fibroblast growth factor receptor 1 Inhibitor fms related receptor tyrosine kinase 3 Inhibitor fms related receptor tyrosine kinase 4 Inhibitor kinase insert domain receptor Inhibitor KIT proto-oncogene，receptor tyrosine kinase Inhibitor platelet derived growth factor receptor beta Inhibitor Raf-1 proto-oncogene，serine/threonine kinase Inhibitor ret proto-oncogene Inhibitor TNNI3 interacting kinase Inhibitor

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基本描述

别名	索拉非尼\|Raf抑制剂\|4-[4-[3-[4-氯-3-(三氟甲基)苯基]脲基]苯氧基]-N-甲基吡啶酰胺
英文别名	Sorafenib\|284461-73-0\|Nexavar\|BAY 43-9006\|sorafenibum\|4-(4-(3-(4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)UREIDO)PHENOXY)-N-METHYLPICOLINAMIDE\|4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide\|Sorafenib free base\|4
规格或纯度	≥99%
英文名称	Sorafenib
生化机理	Sorafenib is a RAF kinase inhibitor which suppresses ERK phosphorylation. Studies indicate that sorafenib induces c-Raf phosphorylation at both Ser-43 and Ser-259. When combined with vitamin K1, phosphorylation is increased at these serine residues. Sorafenib also induces the phosphorylation of PKA. In addition, sorafenib induces c-Met phosphorylation at Tyr-1349, which consequently induces PI3K-Akt phosphorylation. Studies determined that sorafenib inhibits other kinases such as Flk-1 (VEGFR2), PDGFR (platelet-derived growth factor receptor), Flt-3/Flk-2 (FLT3), Ret, and c-Kit. Sorafenib is an inhibitor of Raf-1, Raf-B, PDGFR-βand Flt-4. Its ability to affect the Raf/Mek/Erk pathway makes it useful in cancer research studies.Potent multikinase inhibitor that targets the RAF/MEK/ERK pathway in tumor cells, and tyrosine kinases involved in tumor angiogenesis, oncogenesis, and maintenance of the tumor microenvironment.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂，IC50分别为6 nM, 22 nM和90 nM。还能抑制野生型和V599E突变型BRAF活性。 This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.An inhibitor of tyrosine protein kinases that targets the Raf/Mek/Erk pathway Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia. An inhibitor of tyrosine protein kinases that targets the Raf/Mek/Erk pathway

名称和标识符

IUPAC Name	4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
INCHI	InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
InChi Key	MLDQJTXFUGDVEO-UHFFFAOYSA-N
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
Isomeric SMILES	CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
PubChem CID	216239
分子量	464.83

数据库链接

CAS Registry No.	284461-73-0
DrugBank Ligand	DB00398
Wikipedia	Sorafenib
DiscoveRx TREEspot	Sorafenib\|
PubChem CID	216239
ChEMBL Ligand	CHEMBL1336
RCSB PDB Ligand	BAX
PEP	sorafenib
Reactome Reaction	R-HSA-9702510, R-HSA-9695831, R-HSA-6802938, R-HSA-9669854, R-HSA-9669900, R-HSA-9674430, R-HSA-9674095, R-HSA-9693978, R-HSA-9702623, R-HSA-9669874, R-HSA-9674414
Reactome Drug	R-ALL-9657029
DrugCentral Ligand	2459

化学和物理性质

溶解性	Soluble in DMSO (~20 mg/ml), Hot Methanol, DMF (~20 mg/ml), 1:2 solution of DMSO:PBS(PH 7.2 ) (~0.3 mg/ml), 100% ethanol, and ethyl acetate.
敏感性	对热敏感;对空气敏感

安全和危险性（GHS）

象形图	Health Hazard Environmental Hazard
信号词	Danger
危险声明	H351: Suspected of causing cancer H402: Harmful to aquatic life H410: Very toxic to aquatic life with long lasting effects H372: Causes damage to organs through prolonged or repeated exposure H360: May damage fertility or the unborn child H361: Suspected of damaging fertility or the unborn child H362: May cause harm to breast-fed children
预防措施声明	P273,P280,P405,P501,P264,P260,P270,P391,P263,P203,P318,P319

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三氟甲基在有机合成中的引入

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氟西汀肟菌酯索拉非尼含氟砌块

Trifluoromethyl in organic synthesis

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Sorafenib tosylate Fluoxetine Trifloxystrobin Fluorine block

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参考文献

1. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M et al.. (2004) 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, 64 (19): (7099-109). [PMID:15466206]

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