Tivozanib is a potent and selective VEGFR inhibitor with IC50 of 0.21 nM/0.16 nM/0.24 nM on VEGFR1/2 and 2/3, respectively. It also inhibits PDGFR and c-Kit. c-Met EGFR and IGF-1R activity was weak. Phase 3.

 

Brand: BCM

 

Target: VEGFR; PDGFR; Ephrin Receptor

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: Oral administration of Tivozanib (1 mg/kg) reduced microvessel density and inhibited VEGFR2 phosphorylation in tumor xenograft models.

 

In Vivo: In endothelial cells (IC 50 = 0.16 nM),Tivozanib inhibited VEGF-induced phosphorylation of VEGFR2.

 

Melting Point: >202°C (dec.)

 

Boiling Point: 550.4±50.0 °C(Predicted)

 

pKa: 11.74±0.70(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

Isomeric SMILES: CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl  

 

InChIKey: SPMVMDHWKHCIDT-UHFFFAOYSA-N  

 

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)

 

Attribute
[Chem Name]	1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea
[Synonym]	Tivozanib; AV-951; KRN-951
[CAS No.]	475108-18-0
[MDL No.]	MFCD15146788
[Formula]	C22H19ClN4O5
[Molecular]	454.86
[Form]	White to off-white powder
[Storage]	Keep in dark place. Inert atmosphere. Room temperature

Goods Tag