Axitinib

Synonyms: AG 013736

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.

Axitinib Chemical Structure

Axitinib Chemical Structure

CAS: 319460-85-0

Selleck's Axitinib has been cited by 170 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

Axitinib Related Products

Signaling Pathway

Choose Selective VEGFR Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell Growth Inhibition Assay IC50=0.0000513 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=0.000902 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=0.00682 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.00722 μM SANGER
A204 Growth Inhibition Assay IC50=0.00992 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.10836 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=0.11005 μM SANGER
KU812 Growth Inhibition Assay IC50=0.16577 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.16816 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.17665 μM SANGER
JAR Growth Inhibition Assay IC50=0.23989 μM SANGER
G-361 Growth Inhibition Assay IC50=0.32325 μM SANGER
KG-1 Growth Inhibition Assay IC50=0.37642 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.3932 μM SANGER
K5 Growth Inhibition Assay IC50=0.42127 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.42361 μM SANGER
MFM-223 Growth Inhibition Assay IC50=0.44776 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.51008 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.72113 μM SANGER
SW756 Growth Inhibition Assay IC50=0.99846 μM SANGER
A2780 Growth Inhibition Assay IC50=1.01146 μM SANGER
NB14 Growth Inhibition Assay IC50=1.01801 μM SANGER
H4 Growth Inhibition Assay IC50=1.06422 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=1.06633 μM SANGER
AN3-CA Growth Inhibition Assay IC50=1.08389 μM SANGER
A427 Growth Inhibition Assay IC50=1.10381 μM SANGER
ES7 Growth Inhibition Assay IC50=1.11334 μM SANGER
AGS Growth Inhibition Assay IC50=1.11395 μM SANGER
G-402 Growth Inhibition Assay IC50=1.14694 μM SANGER
ES5 Growth Inhibition Assay IC50=1.17248 μM SANGER
DEL Growth Inhibition Assay IC50=1.25457 μM SANGER
NB10 Growth Inhibition Assay IC50=1.32557 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=1.39042 μM SANGER
D-566MG Growth Inhibition Assay IC50=1.40683 μM SANGER
LXF-289 Growth Inhibition Assay IC50=1.43996 μM SANGER
BT-549 Growth Inhibition Assay IC50=1.56909 μM SANGER
NKM-1 Growth Inhibition Assay IC50=1.60556 μM SANGER
SW780 Growth Inhibition Assay IC50=1.65158 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=1.66383 μM SANGER
HMV-II Growth Inhibition Assay IC50=1.70488 μM SANGER
ALL-PO Growth Inhibition Assay IC50=1.80015 μM SANGER
UACC-257 Growth Inhibition Assay IC50=1.82163 μM SANGER
PA-1 Growth Inhibition Assay IC50=1.82725 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=1.86281 μM SANGER
HSC-4 Growth Inhibition Assay IC50=1.93839 μM SANGER
GCT Growth Inhibition Assay IC50=2.00916 μM SANGER
RT-112 Growth Inhibition Assay IC50=2.13424 μM SANGER
A172 Growth Inhibition Assay IC50=2.13606 μM SANGER
HCE-T Growth Inhibition Assay IC50=2.20598 μM SANGER
YH-13 Growth Inhibition Assay IC50=2.21671 μM SANGER
DK-MG Growth Inhibition Assay IC50=2.23834 μM SANGER
ACN Growth Inhibition Assay IC50=2.23875 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=2.24957 μM SANGER
L-363 Growth Inhibition Assay IC50=2.28061 μM SANGER
HuH-7 Growth Inhibition Assay IC50=2.42165 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=2.47168 μM SANGER
T-24 Growth Inhibition Assay IC50=2.48037 μM SANGER
GOTO Growth Inhibition Assay IC50=2.53013 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=2.59169 μM SANGER
DMS-114 Growth Inhibition Assay IC50=2.66345 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=2.70299 μM SANGER
CHP-212 Growth Inhibition Assay IC50=2.82091 μM SANGER
DMS-273 Growth Inhibition Assay IC50=2.90207 μM SANGER
SF295 Growth Inhibition Assay IC50=3.02597 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=3.15005 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=3.22805 μM SANGER
HCC1806 Growth Inhibition Assay IC50=3.27657 μM SANGER
SF126 Growth Inhibition Assay IC50=3.30017 μM SANGER
SW982 Growth Inhibition Assay IC50=3.33875 μM SANGER
ES8 Growth Inhibition Assay IC50=3.34999 μM SANGER
SCC-4 Growth Inhibition Assay IC50=3.50396 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=3.62616 μM SANGER
EW-11 Growth Inhibition Assay IC50=3.63022 μM SANGER
COR-L105 Growth Inhibition Assay IC50=3.63334 μM SANGER
ES1 Growth Inhibition Assay IC50=3.83094 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=3.91808 μM SANGER
ABC-1 Growth Inhibition Assay IC50=3.93911 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=3.99126 μM SANGER
HCC1395 Growth Inhibition Assay IC50=3.99484 μM SANGER
DU-145 Growth Inhibition Assay IC50=4.12825 μM SANGER
JEG-3 Growth Inhibition Assay IC50=4.15916 μM SANGER
HCC1187 Growth Inhibition Assay IC50=4.21597 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=4.22177 μM SANGER
ONS-76 Growth Inhibition Assay IC50=4.24192 μM SANGER
CAL-27 Growth Inhibition Assay IC50=4.24344 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=4.26658 μM SANGER
HGC-27 Growth Inhibition Assay IC50=4.2966 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=4.31468 μM SANGER
EW-1 Growth Inhibition Assay IC50=4.53014 μM SANGER
SW1573 Growth Inhibition Assay IC50=4.55163 μM SANGER
SNU-423 Growth Inhibition Assay IC50=4.6079 μM SANGER
HOS Growth Inhibition Assay IC50=4.6977 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=4.81418 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=4.89048 μM SANGER
A3-KAW Growth Inhibition Assay IC50=4.97352 μM SANGER
CAS-1 Growth Inhibition Assay IC50=4.99908 μM SANGER
NBsusSR Growth Inhibition Assay IC50=5.03514 μM SANGER
KM12 Growth Inhibition Assay IC50=5.29827 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=5.38185 μM SANGER
EFM-19 Growth Inhibition Assay IC50=5.41737 μM SANGER
D-392MG Growth Inhibition Assay IC50=5.57849 μM SANGER
JVM-3 Growth Inhibition Assay IC50=5.72325 μM SANGER
EW-16 Growth Inhibition Assay IC50=5.75583 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=5.84325 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=5.87918 μM SANGER
COLO-829 Growth Inhibition Assay IC50=5.91504 μM SANGER
KM-H2 Growth Inhibition Assay IC50=5.92395 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=5.92771 μM SANGER
OAW-42 Growth Inhibition Assay IC50=5.98821 μM SANGER
A704 Growth Inhibition Assay IC50=6.10574 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=6.10599 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=6.11248 μM SANGER
MKN45 Growth Inhibition Assay IC50=6.26016 μM SANGER
D-502MG Growth Inhibition Assay IC50=6.28857 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=6.41688 μM SANGER
S-117 Growth Inhibition Assay IC50=6.50267 μM SANGER
HCC1569 Growth Inhibition Assay IC50=6.53737 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=6.54572 μM SANGER
OC-314 Growth Inhibition Assay IC50=6.91159 μM SANGER
SNU-449 Growth Inhibition Assay IC50=7.01072 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=7.19345 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=7.2072 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=7.32386 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=7.4815 μM SANGER
HCC1419 Growth Inhibition Assay IC50=7.53 μM SANGER
HAL-01 Growth Inhibition Assay IC50=7.60644 μM SANGER
HCC2998 Growth Inhibition Assay IC50=7.60743 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=7.63033 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=7.64934 μM SANGER
SW1088 Growth Inhibition Assay IC50=7.65826 μM SANGER
IA-LM Growth Inhibition Assay IC50=7.68613 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=7.6961 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=7.89186 μM SANGER
COLO-800 Growth Inhibition Assay IC50=7.94492 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=8.15783 μM SANGER
D-423MG Growth Inhibition Assay IC50=8.2172 μM SANGER
TE-1 Growth Inhibition Assay IC50=8.44316 μM SANGER
NOS-1 Growth Inhibition Assay IC50=8.51534 μM SANGER
8505C Growth Inhibition Assay IC50=8.64824 μM SANGER
HEC-1 Growth Inhibition Assay IC50=8.78439 μM SANGER
TE-11 Growth Inhibition Assay IC50=8.99551 μM SANGER
CTB-1 Growth Inhibition Assay IC50=9.01433 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=9.02241 μM SANGER
NB17 Growth Inhibition Assay IC50=9.1887 μM SANGER
Becker Growth Inhibition Assay IC50=9.41944 μM SANGER
SN12C Growth Inhibition Assay IC50=9.45234 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=9.60237 μM SANGER
D-283MED Growth Inhibition Assay IC50=9.63072 μM SANGER
D-263MG Growth Inhibition Assay IC50=9.83384 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=9.90127 μM SANGER
T98G Growth Inhibition Assay IC50=9.90203 μM SANGER
HLE Growth Inhibition Assay IC50=9.90909 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=10.0665 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=10.1045 μM SANGER
T47D Growth Inhibition Assay IC50=10.155 μM SANGER
GI-1 Growth Inhibition Assay IC50=10.3533 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=10.4402 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=10.4432 μM SANGER
SCC-15 Growth Inhibition Assay IC50=10.4718 μM SANGER
KS-1 Growth Inhibition Assay IC50=10.6301 μM SANGER
CAL-12T Growth Inhibition Assay IC50=10.6361 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=10.7068 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=11.0328 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=11.2657 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=11.3398 μM SANGER
NH-12 Growth Inhibition Assay IC50=11.5378 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=11.5985 μM SANGER
K-562 Growth Inhibition Assay IC50=11.7248 μM SANGER
ES6 Growth Inhibition Assay IC50=11.8581 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=11.9064 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=11.932 μM SANGER
23132-87 Growth Inhibition Assay IC50=12.0821 μM SANGER
A549 Growth Inhibition Assay IC50=12.3285 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=12.5026 μM SANGER
H9 Growth Inhibition Assay IC50=12.5577 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=12.765 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=12.8258 μM SANGER
HSC-3 Growth Inhibition Assay IC50=12.9276 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=12.9507 μM SANGER
ETK-1 Growth Inhibition Assay IC50=13.0779 μM SANGER
SW1710 Growth Inhibition Assay IC50=13.3641 μM SANGER
COLO-684 Growth Inhibition Assay IC50=13.4541 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=13.5136 μM SANGER
A101D Growth Inhibition Assay IC50=13.5349 μM SANGER
KE-37 Growth Inhibition Assay IC50=13.5887 μM SANGER
SiHa Growth Inhibition Assay IC50=13.8346 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=13.8808 μM SANGER
DB Growth Inhibition Assay IC50=13.9928 μM SANGER
HT-1197 Growth Inhibition Assay IC50=14.0809 μM SANGER
SBC-5 Growth Inhibition Assay IC50=14.1362 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=14.5774 μM SANGER
697 Growth Inhibition Assay IC50=14.627 μM SANGER
OMC-1 Growth Inhibition Assay IC50=14.7888 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=14.8001 μM SANGER
DOK Growth Inhibition Assay IC50=14.9933 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=15.3602 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=15.5095 μM SANGER
LK-2 Growth Inhibition Assay IC50=15.6449 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=15.9075 μM SANGER
GT3TKB Growth Inhibition Assay IC50=16.0676 μM SANGER
GP5d Growth Inhibition Assay IC50=16.342 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=16.4485 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=16.565 μM SANGER
NB7 Growth Inhibition Assay IC50=16.6971 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=16.7326 μM SANGER
8305C Growth Inhibition Assay IC50=16.7877 μM SANGER
CaR-1 Growth Inhibition Assay IC50=16.8111 μM SANGER
D-247MG Growth Inhibition Assay IC50=16.8625 μM SANGER
LoVo Growth Inhibition Assay IC50=16.9488 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=17.1908 μM SANGER
AU565 Growth Inhibition Assay IC50=17.225 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=17.5317 μM SANGER
22RV1 Growth Inhibition Assay IC50=17.5884 μM SANGER
HT-144 Growth Inhibition Assay IC50=17.6598 μM SANGER
HuO9 Growth Inhibition Assay IC50=17.7031 μM SANGER
Daoy Growth Inhibition Assay IC50=17.7184 μM SANGER
SJRH30 Growth Inhibition Assay IC50=17.8489 μM SANGER
CHL-1 Growth Inhibition Assay IC50=17.9249 μM SANGER
J82 Growth Inhibition Assay IC50=17.9635 μM SANGER
COR-L23 Growth Inhibition Assay IC50=18.0011 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=18.2276 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=18.4615 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=18.5697 μM SANGER
ES3 Growth Inhibition Assay IC50=18.5883 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=18.6502 μM SANGER
MN-60 Growth Inhibition Assay IC50=19.0592 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=19.3708 μM SANGER
SW948 Growth Inhibition Assay IC50=19.3934 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=19.4546 μM SANGER
HL-60 Growth Inhibition Assay IC50=20.2141 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=20.4748 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=20.4978 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=20.7967 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=20.906 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=20.9285 μM SANGER
NB12 Growth Inhibition Assay IC50=21.0394 μM SANGER
KY821 Growth Inhibition Assay IC50=21.582 μM SANGER
PSN1 Growth Inhibition Assay IC50=21.6453 μM SANGER
EGI-1 Growth Inhibition Assay IC50=21.7454 μM SANGER
CTV-1 Growth Inhibition Assay IC50=22.3031 μM SANGER
TI-73 Growth Inhibition Assay IC50=22.3498 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=22.4752 μM SANGER
D-542MG Growth Inhibition Assay IC50=22.5558 μM SANGER
ATN-1 Growth Inhibition Assay IC50=22.6439 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=22.8368 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=23.1478 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=23.1944 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=23.4681 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=23.4948 μM SANGER
ESS-1 Growth Inhibition Assay IC50=23.8059 μM SANGER
COR-L88 Growth Inhibition Assay IC50=23.9475 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=24.0312 μM SANGER
HCC1937 Growth Inhibition Assay IC50=24.1 μM SANGER
RS4-11 Growth Inhibition Assay IC50=24.142 μM SANGER
HCC38 Growth Inhibition Assay IC50=24.2394 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=24.6162 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=24.6258 μM SANGER
YAPC Growth Inhibition Assay IC50=24.8214 μM SANGER
NB13 Growth Inhibition Assay IC50=25.2611 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=25.8584 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=26.049 μM SANGER
LS-411N Growth Inhibition Assay IC50=26.2038 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=26.3112 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=26.5454 μM SANGER
HH Growth Inhibition Assay IC50=26.5529 μM SANGER
U-2-OS Growth Inhibition Assay IC50=26.7382 μM SANGER
SF539 Growth Inhibition Assay IC50=26.8018 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=27.086 μM SANGER
A673 Growth Inhibition Assay IC50=27.2102 μM SANGER
WM-115 Growth Inhibition Assay IC50=27.7767 μM SANGER
SW48 Growth Inhibition Assay IC50=27.8005 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=27.8532 μM SANGER
PC-3 Growth Inhibition Assay IC50=27.8941 μM SANGER
UMC-11 Growth Inhibition Assay IC50=27.9343 μM SANGER
U-118-MG Growth Inhibition Assay IC50=28.0123 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=28.0822 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=28.8564 μM SANGER
MC-IXC Growth Inhibition Assay IC50=29.2366 μM SANGER
ES4 Growth Inhibition Assay IC50=29.3172 μM SANGER
BHT-101 Growth Inhibition Assay IC50=29.321 μM SANGER
KP-4 Growth Inhibition Assay IC50=29.516 μM SANGER
CAL-54 Growth Inhibition Assay IC50=29.5445 μM SANGER
5637 Growth Inhibition Assay IC50=29.6421 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=29.7269 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=29.946 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=30.0212 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=30.15 μM SANGER
L-428 Growth Inhibition Assay IC50=30.405 μM SANGER
SW1463 Growth Inhibition Assay IC50=30.5383 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=30.5574 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=30.7702 μM SANGER
YKG-1 Growth Inhibition Assay IC50=31.0263 μM SANGER
A2058 Growth Inhibition Assay IC50=31.1164 μM SANGER
A375 Growth Inhibition Assay IC50=31.1696 μM SANGER
SNB75 Growth Inhibition Assay IC50=31.2435 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=31.4271 μM SANGER
ME-180 Growth Inhibition Assay IC50=31.6542 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=31.8247 μM SANGER
HC-1 Growth Inhibition Assay IC50=32.1446 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=32.1971 μM SANGER
SNU-387 Growth Inhibition Assay IC50=32.3191 μM SANGER
C32 Growth Inhibition Assay IC50=32.3353 μM SANGER
EW-13 Growth Inhibition Assay IC50=32.9408 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=33.5136 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=33.5621 μM SANGER
LU-135 Growth Inhibition Assay IC50=33.801 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=33.9966 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=34.4107 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=34.8515 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=35.2747 μM SANGER
MS-1 Growth Inhibition Assay IC50=35.3038 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=35.5042 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=35.6545 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=36.0496 μM SANGER
EW-22 Growth Inhibition Assay IC50=36.4072 μM SANGER
IGR-1 Growth Inhibition Assay IC50=36.8184 μM SANGER
HT-1080 Growth Inhibition Assay IC50=37.125 μM SANGER
M14 Growth Inhibition Assay IC50=37.1642 μM SANGER
786-0 Growth Inhibition Assay IC50=37.2794 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=37.4501 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=37.9412 μM SANGER
LAN-6 Growth Inhibition Assay IC50=37.9582 μM SANGER
SW620 Growth Inhibition Assay IC50=38.4974 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=39.8205 μM SANGER
Detroit562 Growth Inhibition Assay IC50=40.1268 μM SANGER
HN Growth Inhibition Assay IC50=40.1782 μM SANGER
HCT-15 Growth Inhibition Assay IC50=40.5907 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=40.9157 μM SANGER
A498 Growth Inhibition Assay IC50=41.3015 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=41.4725 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=41.7767 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=41.9821 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=42.2699 μM SANGER
Mo-T Growth Inhibition Assay IC50=42.8958 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=43.4944 μM SANGER
CAL-51 Growth Inhibition Assay IC50=43.5605 μM SANGER
RH-18 Growth Inhibition Assay IC50=43.805 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=43.8347 μM SANGER
HSC-2 Growth Inhibition Assay IC50=44.009 μM SANGER
ML-2 Growth Inhibition Assay IC50=45.2621 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=45.7365 μM SANGER
NB6 Growth Inhibition Assay IC50=46.111 μM SANGER
MCF7 Growth Inhibition Assay IC50=46.5533 μM SANGER
P30-OHK Growth Inhibition Assay IC50=46.8117 μM SANGER
BPH-1 Growth Inhibition Assay IC50=46.9805 μM SANGER
U251 Growth Inhibition Assay IC50=46.994 μM SANGER
MKN1 Growth Inhibition Assay IC50=47.5137 μM SANGER
A431 Growth Inhibition Assay IC50=47.8338 μM SANGER
C8166 Growth Inhibition Assay IC50=49.2039 μM SANGER
HEL Growth Inhibition Assay IC50=49.4064 μM SANGER
RMG-I Growth Inhibition Assay IC50=49.4444 μM SANGER
CAL-72 Growth Inhibition Assay IC50=49.6075 μM SANGER
SW962 Growth Inhibition Assay IC50=49.9332 μM SANGER
MCF7 Antiproliferative assay 5 days Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 0.97 μM. 23829549
MDA-MB-468 Antiproliferative assay 5 days Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 1.3 μM. 23829549
HCC1954 Antiproliferative assay 5 days Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 2.7 μM. 23829549
SKBR3 Antiproliferative assay 5 days Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 3.8 μM. 23829549
MDA-MB-231 Antiproliferative assay 5 days Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 7.3 μM. 23829549
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells after 5 days by SRB assay, GI50 = 2.3 μM. 24867403
MDA-MB-468 Cytotoxicity assay 5 days Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay, GI50 = 2.8 μM. 24867403
SKBR3 Cytotoxicity assay 5 days Cytotoxicity against human SKBR3 cells after 5 days by SRB assay, GI50 = 4.6 μM. 24867403
MDA-MB-231 Cytotoxicity assay 5 days Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay, GI50 = 11 μM. 24867403
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
HUVEC Antiproliferative assay 1 hr Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs by MTT assay, IC50 = 0.0005 μM. ChEMBL
HUVEC Antiproliferative assay 1 hr Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs in presence of albumin by MTT assay, IC50 = 0.0027 μM. ChEMBL
A549 Antiproliferative assay 48 hrs Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay, IC50 = 22.4 μM. ChEMBL
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay, IC50 = 38.7 μM. ChEMBL
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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)
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0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM
In vitro
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]
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 Research 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.

Experimental Result Images Methods Biomarkers Images 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 PARP / cleaved PARP / caspase-3 / cleaved caspase-3 31205508
Immunofluorescence alpha-tubulin 26474283
Growth inhibition assay Cell viability 26474283
In Vivo
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.
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06161558 Not yet recruiting
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
January 12 2024 Phase 1
NCT05969496 Recruiting
Renal Cancer|Kidney Cancer|Renal Cell Carcinoma|Inferior Vena Cava Thrombosis
University of Colorado Denver|Cancer League of Colorado
December 14 2023 Phase 2
NCT05949632 Not yet recruiting
Advanced Solid Tumors
Incyte Corporation
December 15 2023 Phase 1|Phase 2
NCT05904730 Enrolling by invitation
Breast Cancer|Ovarian Cancer|Breast Neoplasms|Ovarian Neoplasms|BRCA Mutation|HER2-positive Breast Cancer|HER2-negative Breast Cancer|HER-2 Protein Overexpression
Lynkcell Europe
July 11 2023 Phase 1
NCT05817903 Recruiting
Metastatic Renal Cell Carcinoma
Consorzio Oncotech|Pfizer
April 18 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 386.47 Formula

C22H18N4OS

CAS No. 319460-85-0 SDF Download Axitinib SDF
Smiles CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 26 mg/mL ( (67.27 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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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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