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Axitinib

Catalog No. S1005 4 Customer Review(s)

Product Citations

5 Product Citation(s)

Axitinib Chemical Structure

Bio Information

It is currently in phase I to III development in a range of solid tumors. In nonclinical and clinical studies, the compound has been shown to inhibit angiogenesis, vascular permeability, and blood flow ^[1,2]. In phase II studies, axitinib showed single-agent activity in a wide range of tumor types, including advanced renal cell carcinoma ^[3] and melanomaas well as improved progression-free survival and overall survival in advanced and metastatic pancreatic cancer when combined with gemcitabine. In transfected or endogenous RTK-expressing cells, axitinib potently blocked growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC50 values of 0.2 and 0.1 to 0.3 nmol/L, respectively. Cellular activity against VEGFR-1 was 1.2 nmol/L (measured in the presence of 2.3% bovine serum albumin), equivalent to an absolute IC50 of -0.1 nmol/L, based on protein binding of axitinib. The potency against murine VEGFR-2 (Flk-1) in Flk-1-transfected NIH-3T3 cells was 0.18 nmol/L, similar to that of its human homologue.

References:

[1] Clin Cancer Res 2008;14:7272-7283

[2] J Clin Oncol 2005;23:5464-5473

[3] Clin Cancer Res 2003;9:327-337

Chemical Information

Molecular Weight (WM):	386.47
Formula:	C₂₂H₁₈N₄OS

Solubility(R.T.:25°C):	DMSO 1mg/mL
	Water <1mg/mL
	Ethanol <1mg/mL

Quality Control

View current batch:

Purity= 99.64% Purity= 99.55% Purity= 99.01% Purity= 99.19% Purity= 99.52% Purity= 97.04% Purity= 99.01% Purity= 99.01% Purity= 99.42% Purity= 99.06%

Research Area

Protein Tyrosine Kinase >> VEGFR >> VEGFR Inhibitors

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Related Antibodies

Product Name	Information

Reactivity: 薛亚红

Axitinib has been referenced in 5 publications.

Metformin accelerates the growth of BRAF V600E-driven melanoma by upregulating VEGF-A.[Martin MJ, et al. Cancer Discov 2012;2(4), 344-355]

PubMed: 22576211

Impact of vegf on astrocytes: Analysis of gap junctional intercellular communication, proliferation, and motility.[Wuestefeld R, et al. Glia 2012;60(6):936-47]

PubMed: 22431192

Axitinib Targeted Cancer Stemlike Cells to Enhance Efficacy of Chemotherapeutic Drugs via Inhibiting the Drug Transport Function of ABCG2.[Wang F, et al. Mol Med 2012;18:887-98]

PubMed: 22549112

Changes in blood vessel maturation in the fibrous cap of the tumor rim.[Naito H, et al. Cancer Sci 2012;103(3):433-8]

PubMed: 22098620

3D models of epithelial-mesenchymal transition in breast cancer metastasis: high-throughput screening assay development,validation, and pilot screen.[Li Q, et al. J Biomol Screen 2011;16(2), 141-154]

PubMed: 21297102

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Average Customer Review

(4 customer reviews)

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Data from [J Biomol Screen 2011;16, 141-154]
Axitinib purchased from Selleck

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Data from [J Biomol Screen 2011;16, 141-154]
Axitinib purchased from Selleck

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;Dr Cheri Pasch of UW Madison
Axitinib purchased from Selleck

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Data from [J Biomol Screen 2011;16, 141-154]
Axitinib purchased from Selleck

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Data from [J Biomol Screen 2011;16, 141-154]

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Data from [J Biomol Screen 2011;16, 141-154]

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