1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Tivozanib (Synonyms: AV-951)

Cat. No.: HY-10977 Purity: 99.46%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
Tivozanib Chemical Structure

Tivozanib Chemical Structure

CAS No. : 475108-18-0

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10 mM * 1 mL in DMSO $66 In-stock
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10 mg $85 In-stock
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100 mg $420 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

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. IC50 value: 30 nM/6.5 nM/15 nM(VEGFR1/2/3) [1] Target: VEGFR1/2/3 in vitro: 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 [1]. 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 [2].

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References
Molecular Weight

454.86

Formula

C₂₂H₁₉ClN₄O₅

CAS No.

475108-18-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Tivozanib
Cat. No.:
HY-10977
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