Free shipping on all orders over $ 500

Tivozanib (AV-951)

Cat. No. M1656
Tivozanib (AV-951) Structure
Synonym:

KRN951; Tivozanib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 65  USD65 In stock
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
25mg USD 180  USD180 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

AV-951 (Tivozanib) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively.AV-951 (Tivozanib) blocks the proliferation and migration of endothelial cells in vitro, and suppresses angiogenesis and growth of human tumor xenografts in vivo.

Protocol (for reference only)
Cell Experiment
Cell lines HUVECs cells line
Preparation method Endothelial cell proliferation. HUVECs were seeded in M-199 (Invitrogen, Carlsbad, CA) containing 5% FBS in collagen-coated 96-well plates (BD Biosciences, Bedford, MA) at a density of 4,000 cells/200 μL/well. After 24 hours, KRN951 was added followed by 20 ng/mL VEGF or 10 ng/mL bFGF, and the cells were cultured for 72 hours. [3H]thymidine (1 μCi/mL) was added and the cells were cultured for a further 12 hours. Cells were then harvested and their radioactivity was measured with a Liquid Scintillation Counter (Wallac 1205 Beta Plate; Perkin-Elmer Life Sciences, Boston, MA).
Concentrations 0~1000nM
Incubation time 72h
Animal Experiment
Animal models human tumor xenografts in athymic rats
Formulation 0.5% methyl cellulose in distilled water
Dosages 0.2 or 1 mg/kg for 14 days
Administration oral gavage
Chemical Information
Molecular Weight 454.86
Formula C22H19ClN4O5
CAS Number 475108-18-0
Solubility (25°C) DMSO 18 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nosov et al J Clin Oncol. Antitumor activity and safety of tivozanib (AV-951) in a phase II randomized discontinuation trial in patients with renal cell carcinoma.

[2] Gupta et al. Expert Opin Pharmacother. Progress and contrasts of the development of tivozanib for therapy of kidney cancer.

[3] Eskens et al. Clin Cancer Res. Biologic and clinical activity of tivozanib (AV-951, KRN-951), a selective inhibitor of VEGF receptor-1, -2, and -3 tyrosine kinases, in a 4-week-on, 2-week-off schedule in patients with advanced solid tumors.

[4] De Luca A et al. IDrugs. Tivozanib, a pan-VEGFR tyrosine kinase inhibitor for the potential treatment of solid tumors.

Related VEGFR/PDGFR Products
Isolinderalactone

Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppressed the expression of B-cell lymphoma 2 (BCL-2), as well as of survivin and X-linked inhibitor of apoptosis protein (XIAP).

Oglufanide

Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus.

KLTWQELYQLKYKGI

KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF.

Protein LMWP

Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity.

CBO-P11

CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis.

  Catalog
Abmole Inhibitor Catalog




Keywords: Tivozanib (AV-951), KRN951; Tivozanib supplier, VEGFR/PDGFR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.