Axitinib (AG 013736)

For research use only.

Licensed by Pfizer Catalog No.S1005

115 publications

Axitinib (AG 013736) Chemical Structure

CAS No. 319460-85-0

Axitinib (AG 013736) 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.

Selleck's Axitinib (AG 013736) has been cited by 115 publications

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Choose Selective VEGFR Inhibitors

Biological Activity

Description Axitinib (AG 013736) 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.
Features Superior as second-line therapy relative to sorafenib (current standard-of-care).
Targets
VEGFR1/FLT1 [1]
(Porcine aorta endothelial cells)
VEGFR2/Flk1 [1]
(Porcine aorta endothelial cells)
VEGFR2/KDR [1]
(Porcine aorta endothelial cells)
VEGFR3 [1]
(Porcine aorta endothelial cells)
PDGFRβ [1]
(Porcine aorta endothelial cells)
0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH70[|JKSzVyPUCuNFAxODVzMzFOwG0> M3vIe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
NCI-H1703 M4\u[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;2TWM2OD1yLkCwNFkxOiEQvF2= NED0fVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
KASUMI-1 NFPvPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOyTWM2OD1yLkCwOlgzKM7:TR?= NXvpXmhGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
CGTH-W-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMEC3NlIh|ryP NWHQW2FERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
A204 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfWXXJxUUN3ME2wMlAxQTl{IN88US=> MnfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
HOP-62 NF;LR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLMTWM2OD1yLkGwPFM3KM7:TR?= MoPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
H-EMC-SS M4\DUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrRS5Q6UUN3ME2wMlEyODB3IN88US=> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlg6QTJ4Lze+V2FPT0WUPD;hQi=>
KU812 NIjYZpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzzTWM2OD1yLkG2OVc4KM7:TR?= NWPVfnNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
EM-2 NGPl[nRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq3TWM2OD1yLkG2PFE3KM7:TR?= M4TzTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzQDl7Mk[vK|5USU6JRWK8M4E,
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JAR Ml;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTpO4lsUUN3ME2wMlI{QTh7IN88US=> NH;OR4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
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MEG-01 NET6[IdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwNEKzOlEh|ryP NW\YWnZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRlODTlfFVlww[T5?
MFM-223 M4roVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe4Wm9KSzVyPUCuOFQ4PzZizszN NID5PFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,W0GQR1XSQE9iRg>?
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NEC8 NV3tN2hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rnSmlEPTB;MD63NlEyOyEQvF2= MknKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQnNCVkeHUkyvZV4>
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NB-EBc1 MlTydWhVWyCjc4PhfS=> NULISZlGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MlzVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 Ml20dWhVWyCjc4PhfS=> MoT1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NYKwcXFVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
HUVEC MXPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHjXPJoyKGi{ MofoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDWSWdHNXO2aX31cIF1\WRiSGXWSWMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDmc4xtd3enZDDifUBi\GSrdHnvckBw\iCYRVfGJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlAxODVizszNMi=> NVz4[IxrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ6OUmyOk8oRkOqRV3CUFww[T5?
HUVEC M{TzRmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NH3aXIoyKGi{ NYixO5psSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBXTUeILYP0bY12dGG2ZXSgTHVXTUNiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSCjZHTpeIlwdiCxZjDWSWdHKG2nYYP1doVlKGGodHXyJFczKGi{czDpckBxemW|ZX7j[UBw\iCjbHL1cYlvKGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFAzPyEQvF2u NF72eXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,S2iHTVLMQE9iRg>?
A549 NX[4UmxtSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGjoPJg1QCCqcoO= MmnvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDWSWdHNXO2aX31cIF1\WRiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA1QCCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDJ{LkSg{txONg>? NInab4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjh7OUK2M{c,S2iHTVLMQE9iRg>?
HepG2 MVPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXPsZWxHPDhiaILz MkfIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDWSWdHNXO2aX31cIF1\WRiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSB|OD63JO69VS5? Mn3KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVI5QTl{Nj:nQmNpTU2ETEyvZV4>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-c-kit / c-kit / p-AKT / AKT / p-ERK / ERK / p-STAT3 / STAT3 / p-STAT5 / STAT5 / p-S6K / S6K / p-S6 / S6; 

PubMed: 31205508     


Immunoblotting analysis of indicated proteins in c-KIT mediated signaling pathways of GIST-T1, GIST-882, GIST-48B, and GIST-5R cell lines.

PARP / cleaved PARP / caspase-3 / cleaved caspase-3; 

PubMed: 31205508     


Immunoblotting analysis of apoptosis-related proteins after axitinib treatment in human GIST cell lines. Imatinib and sunitinib were used as positive controls.

31205508
Immunofluorescence
alpha-tubulin; 

PubMed: 26474283     


Representative images of RCC cells treated as above described, and then immunostained with anti-α-tubulin antibody. Bar: 50 μM

26474283
Growth inhibition assay
Cell viability ; 

PubMed: 26474283     


A. A-498 and Caki-2 RCC cell lines were cultured up to 96 h with different doses of axitinib. Cell viability was determined by MTT assay. Data shown are expressed as mean ± SD of three separate experiments; *p < 0.01 vs vehicle-treated cells. B. RCC cell 䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€

26474283
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.

Protocol

Kinase Assay:

[1]

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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 Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
  • Dosages: 10, 30 or 100 mg/kg
  • Administration: Oral daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL warmed (90.56 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 386.47
Formula

C22H18N4OS

CAS No. 319460-85-0
Storage powder
in solvent
Synonyms N/A
Smiles CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04941768 Recruiting -- Carcinoma Renal Cell Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany|Merck Serono GmbH an affiliate of Merck KGaA Darmstadt Germany August 9 2021 --
NCT04682587 Active not recruiting Drug: Axitinib|Drug: Avelumab|Drug: Pembrolizumab Renal Cell Carcinoma Pfizer February 24 2021 --
NCT04669366 Recruiting Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --
NCT04626128 Recruiting Drug: CLS-AX|Drug: Anti-VEGF Neovascular Age-related Macular Degeneration Clearside Biomedical Inc. December 15 2020 Phase 1|Phase 2
NCT04637204 Completed Drug: Cabozantinib|Drug: Axitinib Renal Cell Carcinoma Ipsen November 24 2020 --

Tech Support

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.

Handling Instructions

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

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

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Frequently Asked Questions

  • Question 1:

    We would like to store at -80℃ after it dissolved in CMC. Do you have any infomation about the suggested concentration in CMC?

  • Answer:

    Axitinib in 0.5% CMC at up to 30mg/ml is a suspension for oral gavage administration only. We don't suggest customer to freeze down the solution but to make fresh if possible. Customer can store it for 1-2 weeks at 4 degree for continuous use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID