Tivozanib (AV-951)

Catalog No. A10101

Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。

Product Citations

Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
Majid Momeny, .et al. Blockade of vascular endothelial growth factor receptors by tivozanib has potential anti-tumour effects on human glioblastoma cells, Sci Rep, 2017, 7: 44075 PMID: 28287096
Nicholas A. Manieri, .et al. Mucosally transplanted mesenchymal stem cells stimulate intestinal healing by promoting angiogenesis, J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
Usui T, .et al. Brain-derived neurotrophic factor promotes angiogenic tube formation through generation of oxidative stress in human vascular endothelial cells., Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679

Technical details

Catalog Num	A10101
M. Wt	454.9
Formula	C22H19ClN4O5
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	475108-18-0
Synonyms	AV-951, AV951
SMILES	CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl

Biological Activity

Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。

Targets

Target	Value
VEGFR2	IC50: 6.5nM
VEGFR3	IC50: 15nM
EphB2	IC50: 24nM
VEGFR1	IC50: 30nM
PDGFRα	IC50: 40nM
PDGFRβ	IC50: 49nM
c-Kit	IC50: 78nM
Tie-2	IC50: 78nM
EphB4	IC50: 480nM
FGFR1	IC50: 530nM
c-Met	IC50: 550nM
Abl	IC50: 620nM
Src	IC50: 960nM
FGFR3	IC50: >1μM
FGFR4	IC50: >1μM
FLT3	IC50: >1μM
EGFR	IC50: >1μM
ErbB2	IC50: >1μM
Insulin Receptor	IC50: >1μM
FAK	IC50: >1μM
ErbB4	IC50: >1μM
IGF-1R	IC50: >1μM
JAK2	IC50: >1μM

Solubility *

In vitro (25°C)	DMSO	19 mg/mL (41.76 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	2% DMSO+30% PEG 300+ddH2O	1 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	21.98 mL	109.91 mL	219.83 mL
0.5 mM	4.4 mL	21.98 mL	43.97 mL
1 mM	2.2 mL	10.99 mL	21.98 mL
5 mM	0.44 mL	2.2 mL	4.4 mL

*The above data is based on the productmolecular weight 454.9 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.