产品名称

英文名称：Tivozanib (AV-951)

同义词

Tivozanib、475108-18-0、AV-951、Tivozanib (AV-951)、KRN-951、AV 951、AV951、1-(2-Chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-3-(5-methylisoxazol-3-yl)urea、KRN951、KIL8951、KRN 951、Kil-8951、N-[2-CHLORO-4-[(6,7-DIMETHOXY-4-QUINOLYL)OXY]PHENYL]-N'-(5-METHYL-3-I

产品性质

CAS编号：475108-18-0

分子式：C22H19ClN4O5

分子量：454.87

PubChem编号：9911830

英文别名：Tivozanib|475108-18-0|AV-951|Tivozanib (AV-951)|KRN-951|AV 951|AV951|1-(2-Chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-3-(5-methylisoxazol-3-yl)urea|KRN951|KIL8951|KRN 951|Kil-8951|N-[2-CHLORO-4-[(6,7-DIMETHOXY-4-QUINOLYL)OXY]PHENYL]-N'-(5-METHYL-3-I

规格或纯度：≥98%

英文名称：Tivozanib (AV-951)

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.

ALogP：4

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

Isomeric 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

ChEMBL Ligand：CHEMBL1289494

CAS Registry No.：475108-18-0

Wikipedia：Tivozanib

RCSB PDB Ligand：AV9

DrugCentral Ligand：5258

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

产品包装