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 in Porcine aorta endothelial cells, respectively.

Price Stock Quantity  
In DMSO USD 64 In stock
USD 70 In stock
USD 120 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Axitinib Chemical Structure

Axitinib Chemical Structure
Molecular Weight: 386.47

Validation & Quality Control

Customer Product Validation(4)

Quality Control & MSDS

Related Compound Libraries

VEGFR Inhibitors with Unique Features

Product Information

  • Compare VEGFR Inhibitors
    Compare VEGFR Products
  • 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 in Porcine aorta endothelial cells, respectively.
Targets VEGFR1/FLT1 [1]
(Porcine aorta endothelial cells)
VEGFR2/Flk1 [1]
(Porcine aorta endothelial cells)
(Porcine aorta endothelial cells)
VEGFR3 [1]
(Porcine aorta endothelial cells)

 View  More

IC50 0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM
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:


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:


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

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:


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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[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.

view more

Clinical Trial Information( data from, updated on 2015-08-29)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02156895 Not yet recruiting Advanced Renal Cell Carcinoma Pfizer December 2015 --
NCT02535533 Not yet recruiting Advanced Metastatic Clear Cell Renal Cell Carcinoma (CCRCC) University of Iowa September 2015 Phase 1
NCT02493751 Not yet recruiting Renal Cell Cancer Pfizer August 2015 Phase 1
NCT02489695 Not yet recruiting Papillary Renal Cell Carcinoma Centre Leon Berard July 2015 Phase 2
NCT02261207 Not yet recruiting Solitary Fibrous Tumor Fondazione IRCCS Istituto Nazionale dei Tumori, Milano November 2014 Phase 2

view more

Chemical Information

Download Axitinib SDF
Molecular Weight (MW) 386.47


CAS No. 319460-85-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms AG 013736
Solubility (25°C) * In vitro DMSO 35 mg/mL warmed (90.56 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.
Chemical Name N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide

Customer Product Validation (4)

Click to enlarge
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).

Click to enlarge
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.

Click to enlarge
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.

Click to enlarge
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.

Product Use Citation (13)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related VEGFR Products

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324)

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • BLZ945

    BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs.

  • Cabozantinib (XL184, BMS-907351)

    Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.

  • Nintedanib (BIBF 1120)

    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

  • Regorafenib (BAY 73-4506)

    Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.

  • Lenvatinib (E7080)

    Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Phase 3.

  • Vandetanib (ZD6474)

    Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay.

  • Pazopanib HCl (GW786034 HCl)

    Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

    Features:A multi-kinase inhibitor.

  • Cediranib (AZD2171)

    Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Phase 3.

Recently Viewed Items

Tags: buy Axitinib | Axitinib ic50 | Axitinib price | Axitinib cost | Axitinib solubility dmso | Axitinib purchase | Axitinib manufacturer | Axitinib research buy | Axitinib order | Axitinib mouse | Axitinib chemical structure | Axitinib mw | Axitinib molecular weight | Axitinib datasheet | Axitinib supplier | Axitinib in vitro | Axitinib cell line | Axitinib concentration | Axitinib nmr
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
Contact Us