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Tivozanib (AV-951)，抑制剂

Tivozanib (AV-951)，抑制剂

规格或纯度: ≥98%

CAS编号: 475108-18-0
分子式: C₂₂H₁₉ClN₄O₅
分子量: 454.87
PubChem编号: 9911830

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货号 (SKU)	包装规格	是否现货	价格	数量
T126012-5mg	5mg	现货
T126012-25mg	25mg	现货
T126012-100mg	100mg	现货

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fms related receptor tyrosine kinase 1 Inhibitor fms related receptor tyrosine kinase 4 Inhibitor kinase insert domain receptor Inhibitor

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基本描述

规格或纯度	≥98%
英文名称	Tivozanib (AV-951)
别名	AV-951;AV951;AV 951
英文别名	AV-951;AV951;AV 951;N-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea
生化机理	AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells [1]. In vivo studies show that AV-951 also decreases the micro vessel density and suppresses VEGFR2 phosphorylation levels in tumor xenografts, especially at a concentration of 1mg/kg (p.o. administration). AV-951 shows almost complete inhibition of tumor xenografts growth (TGI>85%) in athymic rats . Another study in rat peritoneal disseminated tumor model shows that AV-951 could prolong the survival of the tumor-bearing rats with the MST of 53.5 days. AV-951 displays antitumor activity against many human tumor xenografts including lung, breast, colon, ovarian, pancreas and prostate cancer.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Tivozanib (AV-951)是VEGFR抑制剂，对VEGFR1，2和3的IC50分别为30 nM，6.5 nM和15 nM，还能抑制PDGFR和c-Kit，对FGFR-1，Flt3，c-Met，EGFR和IGF-1R的抑制性较低。 Tivozanib (AV-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R.

名称和标识符

IUPAC Name	1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea
INCHI	InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
InChi Key	SPMVMDHWKHCIDT-UHFFFAOYSA-N
Canonical SMILES	CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl
PubChem CID	9911830
分子量	454.87

数据库链接

PubChem CID	9911830
ChEMBL Ligand	CHEMBL1289494
CAS Registry No.	475108-18-0
Wikipedia	Tivozanib
RCSB PDB Ligand	AV9
DrugCentral Ligand	5258

化学和物理性质

溶解性	DMSO ≥36mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

关联配体

Ligand ID	6058
名称	tivozanib
别名	AV-951
类别	Synthetic organic
学名	1-{2-chloro-4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-3-(5-methyl-1,2-oxazol-3-yl)urea
生物活性评价	Tivozanib inhibits all three VEGF receptor tyrosine kinase enzymes with equal potency . The drug formulation contains tivozanib hydrochloride monohydrate (PubChem CID 11547978).
评价	Tivozanib is an oral VEGF receptor tyrosine kinase inhibitor.

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参考文献

1. Musumeci F, Radi M, Brullo C, Schenone S. (2012) Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.. J Med Chem, 55 (24): (10797-822). [PMID:23098265]

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