Axitinib

Licensed by Pfizer Catalog No.S1005 Synonyms: AG 013736

Axitinib Chemical Structure

Molecular Weight(MW): 386.47

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.

Size Price Stock Quantity  
In DMSO USD 64 In stock
USD 70 In stock
USD 120 In stock

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4 Customer Reviews

  • Representative confocal image (10 x objective) of individual spheroids fixed, sectioned, and then stained for vimentin (green) and DNA (DAPI, blue). Vimentin protein expression from sections quantitated from multiple replicate spheroid treatments with U0126 and axitinib using ImageJ software.

    J Biomol Screen, 2011,16: 141-154. Axitinib purchased from Selleck.

    VimPro-Fluc activity in spheroids after 72-h treatment with control modulators of epithelial-mesenchymal transition (EMT) normalized to spheroid viability and compared to vimentin protein expression using Western blot analysis.

    J Biomol Screen, 2011,16: 141-154. Axitinib purchased from Selleck.

  • Secondary assay development. The invasive potential of MDA-MB-231 spheroids was measured using modified Boyden chambers coated with Matrigel™. Invading cells were fixed, stained with DAPI, and quantified by fluorescence microscopy using 5 random fields per filter insert in triplicate. U0126, PF2341066, axitinib, and PKC412 inhibited the invasive potential of MDA-MB-231 spheroids by ~90% as compared to untreated spheroids (UT). ***p ≤ 0.001. IGF1R and dasatinib displayed no statistical difference as compared to UT MDA-MB-231 spheroids.

    J Biomol Screen 2011 16, 141-154. Axitinib purchased from Selleck.

    Axitinib treatment blocks VEGFR2 phosphorylation.

    HUVECs were starved O/N in EBM-2 basal medium with 1% FBS and antibiotic. Cells were pre-treated with Axitinib at 0.1, 1 and 10 nM concentrations. VEGF stimulation was 50 ng/ml for 10 minutes before cells were collected and protein isolated for immunoprecipitation with VEGFR2 followed by immunoblotting with VEGFR-2 and phospho-VEGFR-2.

     

     

    Dr. Cheri Pasch of UW Madison. Axitinib purchased from Selleck.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
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 NV7kT2FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL3TWM2OD1yLkCwNFA2OTNizszN NGK4c2NUSU6JRWK=
NCI-H1703 NEG0eoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHNOotKSzVyPUCuNFAxQTB{IN88US=> M4jnPXNCVkeHUh?=
KASUMI-1 NVnm[VVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHzTWM2OD1yLkCwOlgzKM7:TR?= NHjiXItUSU6JRWK=
CGTH-W-1 NI\sO4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjyOFlLUUN3ME2wMlAxPzJ{IN88US=> MlLwV2FPT0WU
A204 Ml\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMEC5PVIh|ryP MYnTRW5ITVJ?
HOP-62 NFewXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfJR4pKSzVyPUCuNVA5OzZizszN NVfJXIFUW0GQR1XS
H-EMC-SS NVO0cFczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnkTWM2OD1yLkGxNFA2KM7:TR?= NU\VZo16W0GQR1XS
KU812 MnrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwMU[1O|ch|ryP M176dXNCVkeHUh?=
EM-2 NUD3T5V3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDDTWM2OD1yLkG2PFE3KM7:TR?= NWrSSJo5W0GQR1XS
LAMA-84 M4D6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMUe2OlUh|ryP MYXTRW5ITVJ?
JAR Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HsWGlEPTB;MD6yN|k5QSEQvF2= M1XYd3NCVkeHUh?=
G-361 MlfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX2yfpdbUUN3ME2wMlMzOzJ3IN88US=> MlniV2FPT0WU
KG-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17W[2lEPTB;MD6zO|Y1OiEQvF2= NEK3WJJUSU6JRWK=
BV-173 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7hN|BRUUN3ME2wMlM6OzJizszN M4LjN3NCVkeHUh?=
K5 NUHXO45uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe4TWM2OD1yLkSyNVI4KM7:TR?= NVy3[YVzW0GQR1XS
MEG-01 NILtemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfwTWM2OD1yLkSyN|YyKM7:TR?= MlThV2FPT0WU
MFM-223 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwNES3O|Yh|ryP NHXTO4VUSU6JRWK=
BE-13 NILMS25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnKVmlKSzVyPUCuOVExODhizszN NHS1NZlUSU6JRWK=
NEC8 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLCRoVKSzVyPUCuO|IyOTNizszN NXfwcpBZW0GQR1XS
SW756 NYLR[GI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHtUYdKSzVyPUCuPVk5PDZizszN NYnmRpBiW0GQR1XS
A2780 M1XjfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnmbnNEUUN3ME2xMlAyOTR4IN88US=> MXLTRW5ITVJ?
NB14 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XGS2lEPTB;MT6wNVgxOSEQvF2= MWPTRW5ITVJ?
H4 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPEeVZXUUN3ME2xMlA3PDJ{IN88US=> MWrTRW5ITVJ?
SK-OV-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nwZmlEPTB;MT6wOlY{OyEQvF2= M2faZXNCVkeHUh?=
AN3-CA MmfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFwMEizPFkh|ryP NXHuPVN5W0GQR1XS
A427 MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwMUCzPFEh|ryP NIj1V2lUSU6JRWK=
ES7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vabGlEPTB;MT6xNVM{PCEQvF2= MmXyV2FPT0WU
AGS M{\2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\1eGlEPTB;MT6xNVM6PSEQvF2= MVHTRW5ITVJ?
G-402 M1ewOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\vdpZpUUN3ME2xMlE1Pjl2IN88US=> NGDiOmNUSU6JRWK=
ES5 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPtOZRPUUN3ME2xMlE4OjR6IN88US=> Mk\MV2FPT0WU
DEL NVLlSVd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjlOJZKUUN3ME2xMlI2PDV5IN88US=> NWLEOWVUW0GQR1XS
NB10 NHnXV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL0XWlZUUN3ME2xMlMzPTV5IN88US=> MXXTRW5ITVJ?
NCI-H1581 NITTOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LMO2lEPTB;MT6zPVA1OiEQvF2= M4\BcXNCVkeHUh?=
D-566MG NULyNZY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLxTWM2OD1zLkSwOlg{KM7:TR?= M2Xuc3NCVkeHUh?=
LXF-289 NIrRWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u4PWlEPTB;MT60N|k6PiEQvF2= M3P2bXNCVkeHUh?=
BT-549 NIDnSXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\6ZZpQUUN3ME2xMlU3QTB7IN88US=> NGfpc4JUSU6JRWK=
NKM-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGraSGJKSzVyPUGuOlA2PTZizszN Mom2V2FPT0WU
SW780 NXLBVFJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37YeGlEPTB;MT62OVE2QCEQvF2= MYfTRW5ITVJ?
NCI-H292 NVTnfHZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXk[3FyUUN3ME2xMlY3Ozh|IN88US=> MmDpV2FPT0WU
HMV-II NGnuN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHUPJFxUUN3ME2xMlcxPDh6IN88US=> MmTaV2FPT0WU
ALL-PO MoTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLtTWM2OD1zLkiwNFE2KM7:TR?= NHTVNpBUSU6JRWK=
UACC-257 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwOEKxOlMh|ryP MlHaV2FPT0WU
PA-1 NU\S[IZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwOEK3NlUh|ryP M3jSTHNCVkeHUh?=
HD-MY-Z NFfJTVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:5W2lEPTB;MT64OlI5OSEQvF2= MmHWV2FPT0WU
HSC-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\oWWlEPTB;MT65N|g{QSEQvF2= MkLiV2FPT0WU
GCT NV3HcVh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJwMEC5NVYh|ryP NYP5WJBrW0GQR1XS
RT-112 Ml7yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJwMUO0NlQh|ryP NVjHVoZuW0GQR1XS
A172 NV:0No1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr5cG9sUUN3ME2yMlE{PjB4IN88US=> MYLTRW5ITVJ?
HCE-T NXjocVNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXlSGdKSzVyPUKuNlA2QThizszN Ml7kV2FPT0WU
YH-13 NIXES5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwMkG2O|Eh|ryP MUjTRW5ITVJ?
DK-MG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rzbmlEPTB;Mj6yN|g{PCEQvF2= NYHTfWxDW0GQR1XS
ACN M3zqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXVTWM2OD1{LkKzPFc2KM7:TR?= NXfuSpIyW0GQR1XS
VA-ES-BJ NIfWUoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJwMkS5OVch|ryP M3W0S3NCVkeHUh?=
L-363 NYLESmZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXJfpNKSzVyPUKuNlgxPjFizszN MULTRW5ITVJ?
HuH-7 Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrUWFR2UUN3ME2yMlQzOTZ3IN88US=> MXLTRW5ITVJ?
A4-Fuk M4fXZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjMTWM2OD1{LkS3NVY5KM7:TR?= Mlf1V2FPT0WU
T-24 NHPz[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjETWM2OD1{LkS4NFM4KM7:TR?= NHexN|hUSU6JRWK=
GOTO MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnrb|hKSzVyPUKuOVMxOTNizszN NYHu[4FNW0GQR1XS
MV-4-11 NInmRXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfxTWM2OD1{LkW5NVY6KM7:TR?= NVLFeHhoW0GQR1XS
DMS-114 MoDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLPTWM2OD1{Lk[2N|Q2KM7:TR?= NWDQS5ZPW0GQR1XS
MHH-NB-11 NEnCeXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3n2emlEPTB;Mj63NFI6QSEQvF2= M3G1VXNCVkeHUh?=
CHP-212 NILtdJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrKTW5tUUN3ME2yMlgzODlzIN88US=> NH\qUJVUSU6JRWK=
DMS-273 M3jjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnkd|ZKSzVyPUKuPVAzODdizszN NVvQOWJ6W0GQR1XS
SF295 NYO5fphiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XLTWlEPTB;Mz6wNlU6PyEQvF2= NUjwWWZ6W0GQR1XS
NCI-H1563 Mn7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\MZmlEPTB;Mz6xOVAxPSEQvF2= MnK2V2FPT0WU
NCI-H446 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LmOGlEPTB;Mz6yNlgxPSEQvF2= NGHYZohUSU6JRWK=
HCC1806 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTNwMke2OVch|ryP M3;XTXNCVkeHUh?=
SF126 NEHveWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjvRZdbUUN3ME2zMlMxODF5IN88US=> NV\DU5hbW0GQR1XS
SW982 NGLwepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImzXlRKSzVyPUOuN|M5PzVizszN NF7ifmdUSU6JRWK=
ES8 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXpXGt5UUN3ME2zMlM1QTl7IN88US=> M17IOXNCVkeHUh?=
SCC-4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;LT2lEPTB;Mz61NFM6PiEQvF2= MmqzV2FPT0WU
RPMI-8226 NYDDRnNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4juemlEPTB;Mz62NlYyPiEQvF2= MmjrV2FPT0WU
EW-11 M1jrTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTNwNkOwNlIh|ryP NX\KSYJoW0GQR1XS
COR-L105 NHP3fVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\admlEPTB;Mz62N|M{PCEQvF2= M4PrfXNCVkeHUh?=
ES1 MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoKwTWM2OD1|LkizNFk1KM7:TR?= M3Xzb3NCVkeHUh?=
KMOE-2 NE\CfFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknYTWM2OD1|LkmxPFA5KM7:TR?= NUSye2YyW0GQR1XS
ABC-1 M4PuSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXEfGJwUUN3ME2zMlk{QTFzIN88US=> NEjLT2NUSU6JRWK=
NCI-H526 NITlSW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j5RmlEPTB;Mz65PVEzPiEQvF2= Ml3sV2FPT0WU
HCC1395 NYnKWFZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTNwOUm0PFQh|ryP MkHCV2FPT0WU
DU-145 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TMeGlEPTB;ND6xNlgzPSEQvF2= M2e2OnNCVkeHUh?=
JEG-3 NEXPfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;iU2lEPTB;ND6xOVkyPiEQvF2= NX;USmgzW0GQR1XS
HCC1187 NFjiXYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi1TWM2OD12LkKxOVk4KM7:TR?= NUPMfnBXW0GQR1XS
LC-2-ad MlrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fjOGlEPTB;ND6yNlE4PyEQvF2= MlL2V2FPT0WU
ONS-76 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTRwMkSxPVIh|ryP M4XaeXNCVkeHUh?=
CAL-27 MlnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLpfY9KSzVyPUSuNlQ{PDRizszN M2[yR3NCVkeHUh?=
8-MG-BA MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXs[oxKSzVyPUSuNlY3PThizszN MmrUV2FPT0WU
HGC-27 NEnvRXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTRwMkm2OkDPxE1? NFXJSYVUSU6JRWK=
Hs-578-T NU\TephXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTRTWM2OD12LkOxOFY5KM7:TR?= NYqzUlB5W0GQR1XS
EW-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIWzVVlKSzVyPUSuOVMxOTRizszN NYLocmtWW0GQR1XS
SW1573 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPNZWQ2UUN3ME20MlU2OTZ|IN88US=> NYfIdGFsW0GQR1XS
SNU-423 NXjIcZJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrmWm5KSzVyPUSuOlA4QSEQvF2= MV\TRW5ITVJ?
HOS NIiydYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljHTWM2OD12Lk[5O|ch|ryP M{jmWXNCVkeHUh?=
LB1047-RCC M1q4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\oTWM2OD12LkixOFE5KM7:TR?= MXvTRW5ITVJ?
ChaGo-K-1 NEXv[lNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrJbIhKSzVyPUSuPFkxPDhizszN MU\TRW5ITVJ?
A3-KAW MmPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrhTWM2OD12Lkm3N|UzKM7:TR?= NGLyb5pUSU6JRWK=
CAS-1 M3j1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfrc3ZkUUN3ME20Mlk6QTB6IN88US=> M1\DOnNCVkeHUh?=
NBsusSR NGfBTFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3FTWM2OD13LkCzOVE1KM7:TR?= M{LHNnNCVkeHUh?=
KM12 NETNdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTVwMkm4Nlch|ryP M2rYbnNCVkeHUh?=
NCI-H1155 NX;sPWplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfmTWM2OD13LkO4NVg2KM7:TR?= M2fYOHNCVkeHUh?=
EFM-19 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmiyTWM2OD13LkSxO|M4KM7:TR?= NYDaVWRjW0GQR1XS
D-392MG MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDHOmpRUUN3ME21MlU4QDR7IN88US=> NUPR[FRFW0GQR1XS
JVM-3 NWGwVJhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\rTm5YUUN3ME21MlczOzJ3IN88US=> M17hOXNCVkeHUh?=
EW-16 M2nWNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHaW4NKSzVyPUWuO|U2QDNizszN MYrTRW5ITVJ?
KARPAS-45 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTVwOESzNlUh|ryP MkDMV2FPT0WU
NCI-H28 MkjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3YPIhjUUN3ME21Mlg4QTF6IN88US=> M1rEVXNCVkeHUh?=
COLO-829 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjwN|JKSzVyPUWuPVE2ODRizszN NITrOmtUSU6JRWK=
KM-H2 NEjyO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTVwOUKzPVUh|ryP MmrWV2FPT0WU
NCI-H82 M2XuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2xZ3FlUUN3ME21MlkzPzdzIN88US=> MVTTRW5ITVJ?
OAW-42 M3Hy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTVwOUi4NlEh|ryP MX;TRW5ITVJ?
A704 NYnjbpN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDSN|R[UUN3ME22MlExPTd2IN88US=> MWXTRW5ITVJ?
NCI-H1048 NGXyOGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[5WVRuUUN3ME22MlExPTl7IN88US=> M3eyRXNCVkeHUh?=
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HAL-01 NVfxO2w4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5fnBXUUN3ME23MlYxPjR2IN88US=> M3fyd3NCVkeHUh?=
HCC2998 M3T1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTdwNkC3OFMh|ryP NWrXc4pIW0GQR1XS
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SW1088 MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\XR5FKSzVyPUeuOlU5OjZizszN M3nmZXNCVkeHUh?=
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COLO-800 NVrNNnJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPHNmVDUUN3ME23Mlk1PDl{IN88US=> MknVV2FPT0WU
NCI-H2228 NGmyWHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP5cnhxUUN3ME24MlE2Pzh|IN88US=> NIjxeHRUSU6JRWK=
D-423MG M4r5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRThwMkG3NkDPxE1? NHv5PGJUSU6JRWK=
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MDA-MB-231 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDHVHo1UUN3ME2xPE43PTB{IN88US=> MVTTRW5ITVJ?
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... Click to View More Cell Line Experimental Data

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).
  • Formulation: 0.5% carboxymethylcellulose (CMC)
  • Dosages: 10, 30 or 100 mg/kg
  • Administration: Oral daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL (90.56 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 386.47
Formula

C22H18N4OS

CAS No. 319460-85-0
Storage powder
in solvent
Synonyms AG 013736

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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 MSDS / 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
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    C2
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / 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:

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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 Conditions Sponsor/Collaborators Start Date Phases
NCT02156895 Not yet recruiting Advanced Renal Cell Carcinoma Pfizer June 2017 --
NCT02782403 Not yet recruiting Leukemia M.D. Anderson Cancer Center|Pfizer September 2016 Phase 1|Phase 2
NCT02859012 Recruiting Recurrent ACC, metastaticACC, Unreaectable ACC Seoul National University Hospital September 2016 Phase 2
NCT02853331 Recruiting Renal Cell Carcinoma Merck Sharp & Dohme Corp. September 2016 Phase 3
NCT02762513 Recruiting Squamous Cell Carcinoma of the Head and Neck University of Michigan Cancer Center|National Comprehensive Cancer Network August 2016 Phase 2
NCT02684006 Recruiting Renal Cell Cancer Pfizer March 2016 Phase 3

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID