475108-18-0 Tivozanib AKSci X4932
 
 
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  X4932    AKSci Reference Standard
Tivozanib
, 98% (HPLC)
 
AV-951




IDENTITY
CAS Number:475108-18-0
MDL Number:MFCD15146788
MF:C22H19ClN4O5
MW:454.87
SPECIFICATIONS & PROPERTIES
Purity:98% (HPLC)
Spectra:NMR, LCMS, HPLC
Physical Form:Gray to brown powder
Melting Point:208-213°C
Long-Term Storage:Store long-term at 2-8°C

BIOLOGICAL INFO
Solubility:DMSO
Application(s):Selective VEGFR inhibitor for VEGFR1/2/3
Form:Free Base
Research Area:cancer

REVIEW

 Tivozanib also known as AV-951 is an orally bioavailable 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.

REFERENCES
[1]Eskens FA, de Jonge MJ, Bhargava P, Isoe T, Cotreau MM, Esteves B, Hayashi K, Burger H, Thomeer M, van Doorn L, Verweij J.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.Clin Cancer Res. 2011 Nov 15;17(22):7156-63. Epub 2011 Oct 5.
[2] Gupta S, Fishman M.Progress and contrasts of the development of tivozanib for therapy of kidney cancer.Expert Opin Pharmacother. 2011 Dec;12(18):2915-22.
[3] Nosov DA, Esteves B, Lipatov ON, Lyulko AA, Anischenko AA, Chacko RT, Doval DC, Strahs A, Slichenmyer WJ, Bhargava P.Antitumor activity and safety of tivozanib (AV-951) in a phase II randomized discontinuation trial in patients with renal cell carcinoma.J Clin Oncol. 2012 May 10;30(14):1678-85. Epub 2012 Apr 9.
[4] Cook JJ et al. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of July 4, 2020

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


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