Axitinib Licensed by Pfizer

Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.

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Axitinib Chemical Structure

Axitinib Chemical Structure
Molecular Weight: 386.47

Validation & Quality Control

Customer Reviews(4)

Quality Control & MSDS

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Product Information

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  • Research Area
  • Axitinib Mechanism
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
Targets VEGFR1/FLT1 VEGFR2/Flk1 VEGFR2/KDR VEGFR3 PDGFRβ

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IC50 0.1 nM [1] 0.18 nM [1] 0.2 nM [1] 0.1 nM-0.3 nM [1] 1.6 nM [1]
In vitro Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). [2]
In vivo Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
Features Superior as second-line therapy relative to sorafenib (current standard-of-care).

Protocol(Only for Reference)

Kinase Assay:

[1]

Cellular receptor kinase phosphorylation assay Porcine aorta endothelial (PAE) cells, which overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3, which overexpress murine VEGFR2 (Flk-1) or PDGFRα, are generated. The 96-well plates are coated with 100 μL/well of 2.5 μg/mL anti-VEGFR2 antibody, 0.75 μg/mL anti-PDGFRβ antibody, 0.25 μg/mL anti-PDGFRα antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody to prepare ELISA capture plates. Then phosphorylation of RTK is measured by ELISA.

Cell Assay:

[2]

Cell lines HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells
Concentrations 1 nM - 10 μM
Incubation Time 72 hours
Method

Cells are seeded in a 96-well plate at a density of 5 × 104 and cultured for 24 hours. Axitinib is added to the cells at concentrations ranging from 1 nM to 10 μM. Cell viability is measured after 72 hours by MTS tetrazolium substrate and IC50 values are calculated.

Animal Study:

[3]

Animal Models BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
Formulation 0.5% carboxymethylcellulose (CMC)
Dosages 10, 30 or 100 mg/kg
Administration Oral daily
Solubility 0.5% CMC, , 30 mg/mL
* Please note that Selleck 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.
1

References

[1] Hu-Lowe DD, et al. Clin Cancer Res, 2008, 14(22), 7272-7283.

[2] Rossler, J. et al., Int J Cancer, 2011, 128(11), 2748-2758.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01727336 Recruiting Advanced Renal Cell Carcinoma Acceleron Pharma, Inc. 2012-12 Phase 2
NCT01798446 Recruiting Renal Cell Carcinoma|Nonclear Cell|Temsirolimus Resistance Seoul National University Hospital|Pfizer 2013-02 Phase 2
NCT01806064 Recruiting Renal Cell Carcinoma Tracon Pharmaceuticals Inc. 2013-03 Phase 1
NCT01967576 Recruiting Pheochromocytoma|Paraganglioma National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) 2013-10 Phase 2
NCT01999972 Recruiting Advanced Solid Tumors Pfizer 2014-02 Phase 1

Chemical Information

Download Axitinib SDF
Molecular Weight (MW) 386.47
Formula

C22H18N4OS

CAS No. 319460-85-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms AG 013736
Solubility (25°C) * In vitro DMSO 42 mg/mL (108 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 0.5% CMC, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck 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.

Research Area

Customer Reviews (4)


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Rating
Source J Biomol Screen 2011 16, 141-154. Axitinib purchased from Selleck
Method Spheroid staining and sectioning
Cell Lines MDA-MB-231 cells
Concentrations 10 µM
Incubation Time 72 h
Results Significant down-regulation of vimentin protein expression was observed throughout the outer surface of U0126-treated spheroids as visualized by 3d confocal microscopy (Fig. A). to measure the extent of penetration into the spheroid by U0126 or axitinib, spheroids were sectioned and stained for vimentin (Fig. B,C). these results demonstrate that both U0126 and axitinib penetrated into the spheroid, resulting in downregulation of vimentin throughout the whole spheroid by more than 80% as compared to untreated spheroids.

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Rating
Source J Biomol Screen 2011 16, 141-154. Axitinib purchased from Selleck
Method Western blot, Multiplexing VimPro-Fluc-MDA-MB-231 spheroid viability
Cell Lines MDA-MB-231 cells
Concentrations 0-100 µM
Incubation Time
Results When Vimpro-Fluc activity is downregulated between 50% and 70%, there is significant downregulation of vimentin protein expression. When Vimpro-Fluc downregulation reaches ≥70%, then downregulation of vimentin protein expression is more pronounced. of the modulators tested-U0126, dasatinib, axitinib, and pF2341066-all downregulated Vimpro-Fluc activity by≥70%, which correlated with a significant down-reglation of vimentin protein expression. Finally, dose-response curves were generated with both U0126 (IC50 = 2.5 µM) and axitinib (IC50 = 0.25 µM), demonstrating that these small molecules modulate Vimpro-Fluc activity in a dose-dependent manner, indicating that their respective target(s) and signaling pathways play a significant role in maintaining vimentin expression and possibly mesenchymal homeostasis (Fig. B).

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Rating
Source Dr Cheri Pasch of UW Madison. Axitinib purchased from Selleck
Method Western blot
Cell Lines HUVEC cells
Concentrations 0.1-10 nM
Incubation Time
Results Axitinib treatment blocks VEGFR2 phosphorylation.

Click to enlarge
Rating
Source J Biomol Screen 2011 16, 141-154. Axitinib purchased from Selleck
Method Secondary assay
Cell Lines MDA-MB-231 cells
Concentrations 10 µM
Incubation Time
Results U0126, pF2341066, axitinib, and pKC412 caused significant inhibition of the invasive potential of Mda-Mb-231 spheroids. Conversely, dasatinib, a potent inhibitor of vimentin gene expression, did not significantly alter the invasive potential of MDA-MB-231 spheroids.

Product Citations (9)

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