Home Angiogenesis Bcr-Abl inhibitor - FGFR inhibitor - PDGFR inhibitor - VEGFR inhibitor - Src inhibitor - Autophagy inhibitor Ponatinib For research use only.

Ponatinib

Synonyms: AP24534

Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.

Ponatinib Chemical Structure

Ponatinib Chemical Structure

CAS No. 943319-70-8

Purity & Quality Control

Ponatinib Related Products

Signaling Pathway

Bcr-Abl Signaling Pathways

Bcr-Abl Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell Growth Inhibition Assay IC50=0.0000000359 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.0000956 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.000128 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.000165 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.00169 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=0.00217 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.00259 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.00521 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.00655 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=0.00837 μM SANGER
A204 Growth Inhibition Assay IC50=0.01218 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.01833 μM SANGER
AN3-CA Growth Inhibition Assay IC50=0.01873 μM SANGER
BL-70 Growth Inhibition Assay IC50=0.02199 μM SANGER
Daudi Growth Inhibition Assay IC50=0.02537 μM SANGER
KU812 Growth Inhibition Assay IC50=0.02848 μM SANGER
KG-1 Growth Inhibition Assay IC50=0.03294 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=0.04803 μM SANGER
HuO9 Growth Inhibition Assay IC50=0.05448 μM SANGER
EB2 Growth Inhibition Assay IC50=0.05576 μM SANGER
G-402 Growth Inhibition Assay IC50=0.06341 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=0.06379 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=0.07888 μM SANGER
MLMA Growth Inhibition Assay IC50=0.0906 μM SANGER
KM12 Growth Inhibition Assay IC50=0.09737 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=0.09982 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=0.11336 μM SANGER
MFE-296 Growth Inhibition Assay IC50=0.11839 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.12443 μM SANGER
GB-1 Growth Inhibition Assay IC50=0.12512 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.1337 μM SANGER
P30-OHK Growth Inhibition Assay IC50=0.15672 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=0.16266 μM SANGER
MPP-89 Growth Inhibition Assay IC50=0.16933 μM SANGER
SF126 Growth Inhibition Assay IC50=0.17063 μM SANGER
CTB-1 Growth Inhibition Assay IC50=0.17316 μM SANGER
CA46 Growth Inhibition Assay IC50=0.17489 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=0.17732 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=0.17927 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=0.18577 μM SANGER
697 Growth Inhibition Assay IC50=0.18871 μM SANGER
NY Growth Inhibition Assay IC50=0.19287 μM SANGER
T98G Growth Inhibition Assay IC50=0.19318 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=0.19615 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=0.20439 μM SANGER
PF-382 Growth Inhibition Assay IC50=0.20873 μM SANGER
HCT-116 Growth Inhibition Assay IC50=0.21069 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=0.21666 μM SANGER
CCF-STTG1 Growth Inhibition Assay IC50=0.22475 μM SANGER
D-392MG Growth Inhibition Assay IC50=0.23177 μM SANGER
RT-112 Growth Inhibition Assay IC50=0.23795 μM SANGER
MES-SA Growth Inhibition Assay IC50=0.24187 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.24265 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.24367 μM SANGER
NALM-6 Growth Inhibition Assay IC50=0.25543 μM SANGER
TE-15 Growth Inhibition Assay IC50=0.26091 μM SANGER
786-0 Growth Inhibition Assay IC50=0.26228 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=0.26829 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=0.26891 μM SANGER
YT Growth Inhibition Assay IC50=0.26974 μM SANGER
A427 Growth Inhibition Assay IC50=0.27264 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=0.27329 μM SANGER
HuH-7 Growth Inhibition Assay IC50=0.27763 μM SANGER
CAS-1 Growth Inhibition Assay IC50=0.28303 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=0.28419 μM SANGER
ACHN Growth Inhibition Assay IC50=0.29323 μM SANGER
HGC-27 Growth Inhibition Assay IC50=0.29353 μM SANGER
A172 Growth Inhibition Assay IC50=0.29577 μM SANGER
SNU-449 Growth Inhibition Assay IC50=0.29964 μM SANGER
SW982 Growth Inhibition Assay IC50=0.29978 μM SANGER
EFO-21 Growth Inhibition Assay IC50=0.30411 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=0.31164 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.3128 μM SANGER
MFE-280 Growth Inhibition Assay IC50=0.31453 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=0.31466 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=0.31484 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=0.33368 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.33424 μM SANGER
A2780 Growth Inhibition Assay IC50=0.34304 μM SANGER
ACN Growth Inhibition Assay IC50=0.34873 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=0.34989 μM SANGER
BCPAP Growth Inhibition Assay IC50=0.36001 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.36106 μM SANGER
SW1710 Growth Inhibition Assay IC50=0.36455 μM SANGER
OPM-2 Growth Inhibition Assay IC50=0.36473 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=0.38054 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=0.39791 μM SANGER
8305C Growth Inhibition Assay IC50=0.39793 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=0.41586 μM SANGER
HLE Growth Inhibition Assay IC50=0.4186 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=0.42137 μM SANGER
SW780 Growth Inhibition Assay IC50=0.42346 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=0.42415 μM SANGER
H4 Growth Inhibition Assay IC50=0.42451 μM SANGER
SW1088 Growth Inhibition Assay IC50=0.4439 μM SANGER
SF268 Growth Inhibition Assay IC50=0.4486 μM SANGER
RT4 Growth Inhibition Assay IC50=0.45111 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=0.4527 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=0.46195 μM SANGER
CAL-39 Growth Inhibition Assay IC50=0.46519 μM SANGER
CAL-120 Growth Inhibition Assay IC50=0.47643 μM SANGER
ESS-1 Growth Inhibition Assay IC50=0.47821 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.48933 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.49511 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=0.49904 μM SANGER
HOS Growth Inhibition Assay IC50=0.50365 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.51808 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=0.52135 μM SANGER
K052 Growth Inhibition Assay IC50=0.5214 μM SANGER
EHEB Growth Inhibition Assay IC50=0.52182 μM SANGER
MFH-ino Growth Inhibition Assay IC50=0.52351 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=0.52528 μM SANGER
SW1417 Growth Inhibition Assay IC50=0.52781 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=0.54958 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.55735 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.56056 μM SANGER
ECC12 Growth Inhibition Assay IC50=0.56558 μM SANGER
CHL-1 Growth Inhibition Assay IC50=0.57463 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=0.58344 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.58379 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=0.59615 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.61467 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.61715 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=0.62522 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=0.63069 μM SANGER
ES6 Growth Inhibition Assay IC50=0.63295 μM SANGER
BL-41 Growth Inhibition Assay IC50=0.63352 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=0.6481 μM SANGER
HOP-92 Growth Inhibition Assay IC50=0.65672 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=0.6647 μM SANGER
EW-13 Growth Inhibition Assay IC50=0.66779 μM SANGER
647-V Growth Inhibition Assay IC50=0.68148 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=0.69738 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=0.70887 μM SANGER
U-698-M Growth Inhibition Assay IC50=0.71063 μM SANGER
HC-1 Growth Inhibition Assay IC50=0.72405 μM SANGER
8505C Growth Inhibition Assay IC50=0.72741 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=0.73349 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=0.73538 μM SANGER
GAMG Growth Inhibition Assay IC50=0.73653 μM SANGER
CAL-12T Growth Inhibition Assay IC50=0.73877 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=0.77278 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=0.77451 μM SANGER
HPAF-II Growth Inhibition Assay IC50=0.77501 μM SANGER
KGN Growth Inhibition Assay IC50=0.78081 μM SANGER
EFO-27 Growth Inhibition Assay IC50=0.78733 μM SANGER
MEL-HO Growth Inhibition Assay IC50=0.79449 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=0.80529 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=0.80714 μM SANGER
MFM-223 Growth Inhibition Assay IC50=0.81407 μM SANGER
G-361 Growth Inhibition Assay IC50=0.81897 μM SANGER
ETK-1 Growth Inhibition Assay IC50=0.82441 μM SANGER
LU-99A Growth Inhibition Assay IC50=0.84701 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=0.85732 μM SANGER
L-540 Growth Inhibition Assay IC50=0.85801 μM SANGER
U-2-OS Growth Inhibition Assay IC50=0.85846 μM SANGER
HT-1376 Growth Inhibition Assay IC50=0.86051 μM SANGER
COLO-680N Growth Inhibition Assay IC50=0.87933 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=0.89297 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=0.89548 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.92469 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=0.93292 μM SANGER
G-401 Growth Inhibition Assay IC50=0.93695 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.95014 μM SANGER
HCC1395 Growth Inhibition Assay IC50=0.95461 μM SANGER
J82 Growth Inhibition Assay IC50=0.95543 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.96387 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=0.96564 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.9975 μM SANGER
SW872 Growth Inhibition Assay IC50=0.99775 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=1.00494 μM SANGER
HL-60 Growth Inhibition Assay IC50=1.0097 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=1.01252 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=1.01375 μM SANGER
TCCSUP Growth Inhibition Assay IC50=1.01732 μM SANGER
SH-4 Growth Inhibition Assay IC50=1.02244 μM SANGER
MG-63 Growth Inhibition Assay IC50=1.02616 μM SANGER
NB6 Growth Inhibition Assay IC50=1.03109 μM SANGER
CAL-54 Growth Inhibition Assay IC50=1.03959 μM SANGER
DU-145 Growth Inhibition Assay IC50=1.08073 μM SANGER
HCE-4 Growth Inhibition Assay IC50=1.09286 μM SANGER
U-266 Growth Inhibition Assay IC50=1.09633 μM SANGER
HT-1197 Growth Inhibition Assay IC50=1.11438 μM SANGER
EW-1 Growth Inhibition Assay IC50=1.14128 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=1.15368 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=1.1616 μM SANGER
COLO-668 Growth Inhibition Assay IC50=1.1649 μM SANGER
IMR-5 Growth Inhibition Assay IC50=1.16936 μM SANGER
ARH-77 Growth Inhibition Assay IC50=1.22924 μM SANGER
BHT-101 Growth Inhibition Assay IC50=1.2349 μM SANGER
SCC-25 Growth Inhibition Assay IC50=1.23536 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=1.24346 μM SANGER
MKN28 Growth Inhibition Assay IC50=1.25636 μM SANGER
KS-1 Growth Inhibition Assay IC50=1.28269 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=1.28913 μM SANGER
ES7 Growth Inhibition Assay IC50=1.29542 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=1.30615 μM SANGER
HEC-1 Growth Inhibition Assay IC50=1.33755 μM SANGER
ME-180 Growth Inhibition Assay IC50=1.37993 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=1.39595 μM SANGER
IA-LM Growth Inhibition Assay IC50=1.40914 μM SANGER
MN-60 Growth Inhibition Assay IC50=1.43114 μM SANGER
SIMA Growth Inhibition Assay IC50=1.48687 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=1.52054 μM SANGER
ONS-76 Growth Inhibition Assay IC50=1.52311 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=1.53906 μM SANGER
SW48 Growth Inhibition Assay IC50=1.54243 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=1.55741 μM SANGER
SW626 Growth Inhibition Assay IC50=1.5816 μM SANGER
MC-CAR Growth Inhibition Assay IC50=1.58663 μM SANGER
D-336MG Growth Inhibition Assay IC50=1.6294 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=1.63902 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=1.64473 μM SANGER
Calu-1 Growth Inhibition Assay IC50=1.65386 μM SANGER
HCC1806 Growth Inhibition Assay IC50=1.66611 μM SANGER
A101D Growth Inhibition Assay IC50=1.66781 μM SANGER
A704 Growth Inhibition Assay IC50=1.68311 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=1.69854 μM SANGER
RL95-2 Growth Inhibition Assay IC50=1.71463 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=1.72719 μM SANGER
NH-12 Growth Inhibition Assay IC50=1.73427 μM SANGER
AGS Growth Inhibition Assay IC50=1.76358 μM SANGER
NEC8 Growth Inhibition Assay IC50=1.78995 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=1.79721 μM SANGER
A498 Growth Inhibition Assay IC50=1.81282 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=1.81606 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.83767 μM SANGER
D-542MG Growth Inhibition Assay IC50=1.85851 μM SANGER
KNS-42 Growth Inhibition Assay IC50=1.86266 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=1.89074 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=1.90271 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=1.90675 μM SANGER
SNG-M Growth Inhibition Assay IC50=1.95858 μM SANGER
A673 Growth Inhibition Assay IC50=1.97516 μM SANGER
L-428 Growth Inhibition Assay IC50=1.99179 μM SANGER
KM-H2 Growth Inhibition Assay IC50=2.0109 μM SANGER
MC-IXC Growth Inhibition Assay IC50=2.02273 μM SANGER
COLO-678 Growth Inhibition Assay IC50=2.04207 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=2.07851 μM SANGER
HCC38 Growth Inhibition Assay IC50=2.08433 μM SANGER
UACC-62 Growth Inhibition Assay IC50=2.08855 μM SANGER
OAW-42 Growth Inhibition Assay IC50=2.09711 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=2.13817 μM SANGER
COR-L105 Growth Inhibition Assay IC50=2.16373 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=2.18576 μM SANGER
A431 Growth Inhibition Assay IC50=2.19019 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=2.23951 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=2.33184 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=2.33235 μM SANGER
ST486 Growth Inhibition Assay IC50=2.41048 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=2.41271 μM SANGER
RKO Growth Inhibition Assay IC50=2.42029 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=2.44029 μM SANGER
639-V Growth Inhibition Assay IC50=2.45382 μM SANGER
ES3 Growth Inhibition Assay IC50=2.49737 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=2.56826 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=2.5821 μM SANGER
SN12C Growth Inhibition Assay IC50=2.58487 μM SANGER
COLO-679 Growth Inhibition Assay IC50=2.58605 μM SANGER
U-118-MG Growth Inhibition Assay IC50=2.58872 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=2.64807 μM SANGER
HCT-15 Growth Inhibition Assay IC50=2.68792 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=2.70747 μM SANGER
K5 Growth Inhibition Assay IC50=2.71845 μM SANGER
MKN45 Growth Inhibition Assay IC50=2.73366 μM SANGER
DMS-273 Growth Inhibition Assay IC50=2.75632 μM SANGER
C8166 Growth Inhibition Assay IC50=2.78513 μM SANGER
Calu-3 Growth Inhibition Assay IC50=2.78969 μM SANGER
SNB75 Growth Inhibition Assay IC50=2.88535 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=2.90191 μM SANGER
C-4-II Growth Inhibition Assay IC50=2.91353 μM SANGER
MS-1 Growth Inhibition Assay IC50=2.96769 μM SANGER
A375 Growth Inhibition Assay IC50=3.08184 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=3.08882 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=3.10995 μM SANGER
LN-405 Growth Inhibition Assay IC50=3.13518 μM SANGER
BOKU Growth Inhibition Assay IC50=3.14256 μM SANGER
TE-10 Growth Inhibition Assay IC50=3.17362 μM SANGER
MKN1 Growth Inhibition Assay IC50=3.18483 μM SANGER
M059J Growth Inhibition Assay IC50=3.20173 μM SANGER
GOTO Growth Inhibition Assay IC50=3.22039 μM SANGER
DK-MG Growth Inhibition Assay IC50=3.25976 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=3.2658 μM SANGER
NB12 Growth Inhibition Assay IC50=3.33224 μM SANGER
DOK Growth Inhibition Assay IC50=3.36186 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=3.36287 μM SANGER
AM-38 Growth Inhibition Assay IC50=3.38051 μM SANGER
GR-ST Growth Inhibition Assay IC50=3.45732 μM SANGER
D-247MG Growth Inhibition Assay IC50=3.48263 μM SANGER
TE-8 Growth Inhibition Assay IC50=3.49333 μM SANGER
LS-411N Growth Inhibition Assay IC50=3.49692 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=3.56433 μM SANGER
SF295 Growth Inhibition Assay IC50=3.61552 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=3.65921 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=3.6626 μM SANGER
PC-14 Growth Inhibition Assay IC50=3.66437 μM SANGER
EW-7 Growth Inhibition Assay IC50=3.67693 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=3.71837 μM SANGER
TE-441-T Growth Inhibition Assay IC50=3.73028 μM SANGER
NCI-H1618 Growth Inhibition Assay IC50=3.81875 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=3.81916 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=3.83126 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=3.87009 μM SANGER
KLE Growth Inhibition Assay IC50=3.9067 μM SANGER
Becker Growth Inhibition Assay IC50=3.92849 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=4.07974 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=4.08306 μM SANGER
RS4-11 Growth Inhibition Assay IC50=4.11255 μM SANGER
D-502MG Growth Inhibition Assay IC50=4.16997 μM SANGER
GI-1 Growth Inhibition Assay IC50=4.28299 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=4.3378 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=4.48149 μM SANGER
LOUCY Growth Inhibition Assay IC50=4.48432 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=4.51793 μM SANGER
SCC-9 Growth Inhibition Assay IC50=4.53172 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=4.59293 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=4.66771 μM SANGER
SR Growth Inhibition Assay IC50=4.70048 μM SANGER
CMK Growth Inhibition Assay IC50=4.72101 μM SANGER
COLO-829 Growth Inhibition Assay IC50=4.77043 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=4.83281 μM SANGER
5637 Growth Inhibition Assay IC50=4.90487 μM SANGER
A253 Growth Inhibition Assay IC50=4.97708 μM SANGER
NB10 Growth Inhibition Assay IC50=5.07497 μM SANGER
SF539 Growth Inhibition Assay IC50=5.09959 μM SANGER
HAL-01 Growth Inhibition Assay IC50=5.14645 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=5.16925 μM SANGER
DEL Growth Inhibition Assay IC50=5.27582 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=5.35007 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=5.35107 μM SANGER
HMV-II Growth Inhibition Assay IC50=5.3943 μM SANGER
NB69 Growth Inhibition Assay IC50=5.39631 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=5.43364 μM SANGER
SNU-475 Growth Inhibition Assay IC50=5.47171 μM SANGER
RXF393 Growth Inhibition Assay IC50=5.48494 μM SANGER
CAL-51 Growth Inhibition Assay IC50=5.62853 μM SANGER
SW1573 Growth Inhibition Assay IC50=5.63534 μM SANGER
GCT Growth Inhibition Assay IC50=5.75929 μM SANGER
COR-L88 Growth Inhibition Assay IC50=5.76846 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=5.87536 μM SANGER
NB5 Growth Inhibition Assay IC50=5.9244 μM SANGER
GMS-10 Growth Inhibition Assay IC50=5.96861 μM SANGER
CHP-212 Growth Inhibition Assay IC50=6.48267 μM SANGER
TE-11 Growth Inhibition Assay IC50=6.55182 μM SANGER
SW962 Growth Inhibition Assay IC50=6.65774 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=6.82011 μM SANGER
C-33-A Growth Inhibition Assay IC50=6.91688 μM SANGER
IGR-1 Growth Inhibition Assay IC50=6.97826 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=7.15406 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=7.27046 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=7.28605 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=7.29571 μM SANGER
MKN7 Growth Inhibition Assay IC50=7.37235 μM SANGER
SW620 Growth Inhibition Assay IC50=7.38205 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=7.40798 μM SANGER
TE-6 Growth Inhibition Assay IC50=7.44908 μM SANGER
D-263MG Growth Inhibition Assay IC50=7.45762 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=7.77029 μM SANGER
DSH1 Growth Inhibition Assay IC50=7.79762 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=8.00694 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=8.07508 μM SANGER
SW948 Growth Inhibition Assay IC50=8.10744 μM SANGER
LK-2 Growth Inhibition Assay IC50=8.12833 μM SANGER
HT-1080 Growth Inhibition Assay IC50=8.13175 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=8.193 μM SANGER
HSC-4 Growth Inhibition Assay IC50=8.2872 μM SANGER
LXF-289 Growth Inhibition Assay IC50=8.35943 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=8.36304 μM SANGER
no-11 Growth Inhibition Assay IC50=8.47133 μM SANGER
SNU-387 Growth Inhibition Assay IC50=8.63246 μM SANGER
Detroit562 Growth Inhibition Assay IC50=8.75455 μM SANGER
SW954 Growth Inhibition Assay IC50=8.76832 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=8.7894 μM SANGER
TE-9 Growth Inhibition Assay IC50=8.81062 μM SANGER
NB13 Growth Inhibition Assay IC50=8.83796 μM SANGER
BPH-1 Growth Inhibition Assay IC50=8.85081 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=8.87892 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=8.89926 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=8.97732 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=8.98606 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=9.0346 μM SANGER
GP5d Growth Inhibition Assay IC50=9.06313 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=9.44731 μM SANGER
EW-16 Growth Inhibition Assay IC50=9.44848 μM SANGER
Calu-6 Growth Inhibition Assay IC50=9.49703 μM SANGER
LC4-1 Growth Inhibition Assay IC50=9.6257 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=9.68766 μM SANGER
BC-1 Growth Inhibition Assay IC50=9.7899 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=9.79495 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=9.84933 μM SANGER
SBC-1 Growth Inhibition Assay IC50=10.072 μM SANGER
TUR Growth Inhibition Assay IC50=10.1657 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=10.2114 μM SANGER
C3A Growth Inhibition Assay IC50=10.3179 μM SANGER
SW1990 Growth Inhibition Assay IC50=10.328 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=10.5693 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=10.777 μM SANGER
OAW-28 Growth Inhibition Assay IC50=10.9888 μM SANGER
HN Growth Inhibition Assay IC50=11.1131 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=11.1576 μM SANGER
Daoy Growth Inhibition Assay IC50=11.4336 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=11.7195 μM SANGER
MCF7 Growth Inhibition Assay IC50=11.8126 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=11.9091 μM SANGER
IPC-298 Growth Inhibition Assay IC50=11.9383 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=12.0218 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=12.1141 μM SANGER
SJRH30 Growth Inhibition Assay IC50=12.2299 μM SANGER
DMS-53 Growth Inhibition Assay IC50=12.2649 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=12.3357 μM SANGER
RVH-421 Growth Inhibition Assay IC50=12.4904 μM SANGER
Raji Growth Inhibition Assay IC50=12.614 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=12.6444 μM SANGER
EFE-184 Growth Inhibition Assay IC50=12.7106 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=12.9247 μM SANGER
BHY Growth Inhibition Assay IC50=13.339 μM SANGER
YKG-1 Growth Inhibition Assay IC50=13.3749 μM SANGER
EW-3 Growth Inhibition Assay IC50=13.7163 μM SANGER
HCC1143 Growth Inhibition Assay IC50=13.7437 μM SANGER
REH Growth Inhibition Assay IC50=13.8982 μM SANGER
CESS Growth Inhibition Assay IC50=13.9489 μM SANGER
EFM-19 Growth Inhibition Assay IC50=14.1112 μM SANGER
U031 Growth Inhibition Assay IC50=14.4085 μM SANGER
ES1 Growth Inhibition Assay IC50=14.4851 μM SANGER
HSC-3 Growth Inhibition Assay IC50=14.6215 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=14.7068 μM SANGER
A388 Growth Inhibition Assay IC50=14.7556 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=14.773 μM SANGER
Capan-2 Growth Inhibition Assay IC50=14.786 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=14.8862 μM SANGER
HEL Growth Inhibition Assay IC50=14.8997 μM SANGER
BEN Growth Inhibition Assay IC50=14.9766 μM SANGER
MC116 Growth Inhibition Assay IC50=15.1599 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=15.2317 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=15.5305 μM SANGER
ABC-1 Growth Inhibition Assay IC50=15.8033 μM SANGER
EW-18 Growth Inhibition Assay IC50=15.9979 μM SANGER
BC-3 Growth Inhibition Assay IC50=16.0562 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=16.0667 μM SANGER
SCC-15 Growth Inhibition Assay IC50=16.2825 μM SANGER
TT Growth Inhibition Assay IC50=16.5888 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=16.8273 μM SANGER
C32 Growth Inhibition Assay IC50=16.9717 μM SANGER
SBC-5 Growth Inhibition Assay IC50=17.1479 μM SANGER
NB1 Growth Inhibition Assay IC50=17.3188 μM SANGER
EB-3 Growth Inhibition Assay IC50=17.576 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=17.7035 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=17.7526 μM SANGER
WM-115 Growth Inhibition Assay IC50=17.8085 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=17.9546 μM SANGER
CAL-33 Growth Inhibition Assay IC50=18.2781 μM SANGER
SCC-4 Growth Inhibition Assay IC50=18.3229 μM SANGER
RMG-I Growth Inhibition Assay IC50=18.6947 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=18.7746 μM SANGER
A2058 Growth Inhibition Assay IC50=18.8255 μM SANGER
HCC70 Growth Inhibition Assay IC50=19.3894 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=19.4148 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=19.5899 μM SANGER
CAL-72 Growth Inhibition Assay IC50=19.6737 μM SANGER
L-363 Growth Inhibition Assay IC50=20.0212 μM SANGER
SNU-423 Growth Inhibition Assay IC50=20.1043 μM SANGER
PLC-PRF-5 Growth Inhibition Assay IC50=20.3906 μM SANGER
SW1463 Growth Inhibition Assay IC50=20.4525 μM SANGER
769-P Growth Inhibition Assay IC50=20.6769 μM SANGER
DMS-79 Growth Inhibition Assay IC50=20.849 μM SANGER
Saos-2 Growth Inhibition Assay IC50=20.9556 μM SANGER
CHP-126 Growth Inhibition Assay IC50=21.4462 μM SANGER
SW837 Growth Inhibition Assay IC50=21.4939 μM SANGER
SHP-77 Growth Inhibition Assay IC50=21.6122 μM SANGER
DB Growth Inhibition Assay IC50=21.6142 μM SANGER
ES5 Growth Inhibition Assay IC50=21.6864 μM SANGER
COR-L23 Growth Inhibition Assay IC50=21.8051 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=21.8982 μM SANGER
T84 Growth Inhibition Assay IC50=21.9819 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=22.5363 μM SANGER
LU-165 Growth Inhibition Assay IC50=22.554 μM SANGER
COLO-792 Growth Inhibition Assay IC50=22.7111 μM SANGER
CAL-62 Growth Inhibition Assay IC50=22.7517 μM SANGER
HCE-T Growth Inhibition Assay IC50=22.8606 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=23.0344 μM SANGER
SiHa Growth Inhibition Assay IC50=23.3968 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=24.0641 μM SANGER
U251 Growth Inhibition Assay IC50=24.0668 μM SANGER
LoVo Growth Inhibition Assay IC50=24.9282 μM SANGER
GCIY Growth Inhibition Assay IC50=25.2877 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=25.3316 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=25.3498 μM SANGER
PA-1 Growth Inhibition Assay IC50=25.6833 μM SANGER
OE33 Growth Inhibition Assay IC50=25.6853 μM SANGER
HT-29 Growth Inhibition Assay IC50=25.7879 μM SANGER
RCM-1 Growth Inhibition Assay IC50=25.9656 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=25.9911 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=26.1708 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=26.2738 μM SANGER
COLO-824 Growth Inhibition Assay IC50=26.4002 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=26.5675 μM SANGER
EGI-1 Growth Inhibition Assay IC50=27.2698 μM SANGER
LAN-6 Growth Inhibition Assay IC50=27.3598 μM SANGER
GAK Growth Inhibition Assay IC50=27.4225 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=27.5053 μM SANGER
JVM-2 Growth Inhibition Assay IC50=27.6622 μM SANGER
UACC-257 Growth Inhibition Assay IC50=27.6878 μM SANGER
SW1783 Growth Inhibition Assay IC50=27.7783 μM SANGER
HT-3 Growth Inhibition Assay IC50=28.2166 μM SANGER
RL Growth Inhibition Assay IC50=28.5911 μM SANGER
TK10 Growth Inhibition Assay IC50=28.6535 μM SANGER
HT55 Growth Inhibition Assay IC50=29.0565 μM SANGER
BT-20 Growth Inhibition Assay IC50=29.0586 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=29.1831 μM SANGER
HSC-2 Growth Inhibition Assay IC50=29.3001 μM SANGER
COLO-205 Growth Inhibition Assay IC50=29.3944 μM SANGER
GT3TKB Growth Inhibition Assay IC50=29.6877 μM SANGER
T47D Growth Inhibition Assay IC50=29.8582 μM SANGER
OMC-1 Growth Inhibition Assay IC50=30.1919 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=31.2659 μM SANGER
JEG-3 Growth Inhibition Assay IC50=31.3561 μM SANGER
RD Growth Inhibition Assay IC50=31.5115 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=32.4179 μM SANGER
DMS-114 Growth Inhibition Assay IC50=32.4182 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=32.6501 μM SANGER
CAL-148 Growth Inhibition Assay IC50=32.6665 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=32.9338 μM SANGER
ES4 Growth Inhibition Assay IC50=33.1705 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=33.4601 μM SANGER
LP-1 Growth Inhibition Assay IC50=34.09 μM SANGER
AU565 Growth Inhibition Assay IC50=34.5069 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=35.1426 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=35.171 μM SANGER
SW13 Growth Inhibition Assay IC50=35.4076 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=35.5598 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=35.6691 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=36.0294 μM SANGER
COR-L279 Growth Inhibition Assay IC50=36.1981 μM SANGER
ATN-1 Growth Inhibition Assay IC50=36.8516 μM SANGER
HCC2998 Growth Inhibition Assay IC50=36.8571 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=36.8675 μM SANGER
DV-90 Growth Inhibition Assay IC50=36.9067 μM SANGER
ES8 Growth Inhibition Assay IC50=36.9318 μM SANGER
YAPC Growth Inhibition Assay IC50=36.9654 μM SANGER
HCC1599 Growth Inhibition Assay IC50=37.1618 μM SANGER
UMC-11 Growth Inhibition Assay IC50=37.2503 μM SANGER
THP-1 Growth Inhibition Assay IC50=37.2868 μM SANGER
OCUB-M Growth Inhibition Assay IC50=37.2891 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=37.3233 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=37.3624 μM SANGER
COLO-800 Growth Inhibition Assay IC50=37.567 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=38.3492 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=38.4489 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=38.7344 μM SANGER
ECC4 Growth Inhibition Assay IC50=39.0814 μM SANGER
KP-4 Growth Inhibition Assay IC50=39.1235 μM SANGER
NCI-H2227 Growth Inhibition Assay IC50=39.3949 μM SANGER
22RV1 Growth Inhibition Assay IC50=39.8398 μM SANGER
SAS Growth Inhibition Assay IC50=40.096 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=40.1828 μM SANGER
MDA-MB-468 Growth Inhibition Assay IC50=40.5346 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=41.2075 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=41.2179 μM SANGER
23132-87 Growth Inhibition Assay IC50=41.2732 μM SANGER
HCC1569 Growth Inhibition Assay IC50=41.2885 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=42.1886 μM SANGER
K-562 Growth Inhibition Assay IC50=42.2854 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=42.8974 μM SANGER
SW756 Growth Inhibition Assay IC50=43.0388 μM SANGER
M14 Growth Inhibition Assay IC50=43.3189 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=43.464 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=43.762 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=43.9099 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=43.9281 μM SANGER
PC-3 Growth Inhibition Assay IC50=44.4347 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=44.4474 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=44.708 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=44.7937 μM SANGER
TE-5 Growth Inhibition Assay IC50=45.9581 μM SANGER
EW-24 Growth Inhibition Assay IC50=46.1723 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=46.2155 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=46.7185 μM SANGER
EW-11 Growth Inhibition Assay IC50=46.9373 μM SANGER
KALS-1 Growth Inhibition Assay IC50=47.2066 μM SANGER
BT-474 Growth Inhibition Assay IC50=47.4216 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=47.888 μM SANGER
HCC2157 Growth Inhibition Assay IC50=48.076 μM SANGER
HCC1954 Growth Inhibition Assay IC50=48.1704 μM SANGER
FADU Growth Inhibition Assay IC50=48.3031 μM SANGER
S-117 Growth Inhibition Assay IC50=48.3815 μM SANGER
LS-1034 Growth Inhibition Assay IC50=48.7067 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=49.5543 μM SANGER
LU-134-A Growth Inhibition Assay IC50=49.8085 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=49.8087 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Targets
Abl [1]
(Cell-free assay)		 PDGFRα [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 c-Src [1]
(Cell-free assay)		 Click to View More Targets
0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM
In vitro
In vitro AP24534 potently inhibits native Abl, AblT315I, and other clinically important Abl kinase domain mutants with IC50 of 0.30 nM–2 nM. AP24534 doesn't inhibit Aurora kinase family members, nor does it inhibit insulin receptor or CDK2/cyclin E. AP24534 inhibits proliferation of Ba/F3 cells expressing Bcr-Abl with IC50 of 0.5 nM, as well as Ba/F3 cells expressing a range of Bcr-Abl mutants with IC50 of 0.5 nM–36 nM. The inhibition of proliferation by AP24534 is correlated with induction of apoptosis. [1-2] In leukemic cell lines containing activated forms of FLT3, KIT, FGFR1, and PDGFRα receptors, AP24534 potently inhibits receptor phosphorylation and cellular proliferation with IC50 of 0.3 nM to 20 nM. In MV4-11 (FLT3-ITD(+/+)) but not RS4;11 (FLT3-ITD(–/–)) AML cells, AP24534 inhibits FLT3 signaling and induced apoptosis at less than 10 nM. AP24534 inhibits viability of primary leukemic blasts from a FLT3-ITD positive AML patient with IC50 of 4 nM but not those from patients with AML expressing native FLT3. [3] In Ba/F3 cells engineered to express activated FGFR1-4, AP24534 potently inhibits FGFR-mediated signaling and viability with IC50 lower than 40 nM. In cell lines representing multiple tumor types (endometrial, bladder, gastric, breast, lung, and colon), and containing FGFRs dysregulated by a variety of mechanisms, AP24534 inhibits FGFR-mediated signaling with IC50 less than 40 nM and inhibits cell growth with IC50 of 7 nM–181 nM. [4]
Kinase Assay Peptide substrate phosphorylation assays with GST-Abl kinase domains
The effect of AP24534 (0-320 nM) on GST-Abl kinase activity is assessed by using a synthetic peptide substrate (Abltide: EAIYAAPFAKKK). Assays are carried out at 30 °C for 15 min in 25 μL reaction mixture: 8 mM MOPS (pH 7), 0.2 mM EDTA, 50 μM Abltide, 30 mM MgCl2, 10 mM β-glycerol phosphate, 1 mM EGTA, 0.002% Brij-35, 0.4 mM DTT, 0.2 mg/mL BSA, 0.4 mM sodium orthovanadate, 10 nM WT or mutant GST-Abl kinase, and 100 µM ATP/γ-32[P]ATP (5000 cpm/pmol). Reactions are terminated by transferring a portion of the reaction mixture onto a p81 phosphocellulose filter and immersing in 0.75% phosphoric acid. Filters are washed 3 times in 0.75% phosphoric acid, rinsed in acetone, and air dried; phosphate incorporation is determined by scintillation counting. All results are corrected for background binding to the filters, as determined by omitting peptide substrate from the kinase reaction. Time course experiments to establish the linear range of enzymatic activity precedes kinase assays.
Cell Research Cell lines Ba/F3 cells expressing Bcr-Abl or a range of single mutations in the kinase domain of Bcr-Abl
Concentrations 0-625 nM
Incubation Time 72 hours
Method Ba/F3 cell lines are distributed in 96-well plates (4 × 103 cells/well) and incubated with AP24534 for 72 hours. Proliferation is measured using a methanethiosulfonate (MTS)-based viability assay (CellTiter96 Aqueous One Solution). All values are normalized to the control wells with no drug. IC50 values are reported as the mean of three independent experiments performed in quadruplicat
Experimental Result Images Methods Biomarkers Images PMID
Western blot ABL β-catenin β-catenin Mcl-1 / Survivin / Bcl-Xl / XIAP / Bax / Bcl-2 / Bim AIF / Cyto C PARP / Caspase-3 / Active Caspase-3 p-PDGFRα / PDGFRα PI3K p85 / p-PI3K / p-PDK1 / PDK1 / p-mTOR / mTOR p-JAK2 / JAK2 / p-STAT3 / STAT3 p-p38 MAPK / p38 MAPK c-Jun / p-JNK(T183/Y185) / JNK p-MEK / MEK / p-ERK / ERK RAD51 p-Rb(S807/811) / Rb / CDK4 / CDK6 / Cyclin D1 / CDK2 / Cyclin E1 cleaved caspase-3 / cleaved caspase-7 / BAX / Bcl-2 pFGFR1(pY20) / FGFR1 pSrc / Src / pPlcg / Plcg / pStat5 / Stat5 19878872
Growth inhibition assay Cell viability 30174789
In Vivo
In vivo In a mouse xenograft model of Ba/F3 cells expressing native Bcr-Abl, AP24534 (2.5 mg/kg and 5 mg/kg) prolongs mice median survival. In the xenograft model of Ba/F3 Bcr-AblT315I, AP24534 (10 mg/kg–50 mg/kg) significantly suppresses tumor growth. AP24534 (30 mg/kg) decreases the phosphorylated Bcr-Abl and phosphorylated CrkL levels in the tumors. [2]
Animal Research Animal Models Mouse xenograft models of Ba/F3 cells expressing Bcr-Abl or Bcr-AblT315I
Dosages 2.5 mg/kg and 5 mg/kg for Ba/F3 Bcr-Abl; 2.5 mg/kg–50 mg/kg for Ba/F3 Bcr-AblT315I
Administration Oral gavage once daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05306301 Recruiting
Chemotherapy|Leukemia Acute Lymphoblastic
Gruppo Italiano Malattie EMatologiche dell''Adulto
 October 5 2022 Phase 2
NCT05268003 Recruiting
Acute Lymphoblastic Leukemia|Leukemia
M.D. Anderson Cancer Center
 June 7 2022 Phase 2

Chemical Information & Solubility

Molecular Weight 532.56 Formula

C29H27F3N6O
CAS No. 943319-70-8 SDF Download Ponatinib SDF
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CN=C5N4N=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (137.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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:
Is the pre-solubilized inhibitor suitable for in vivo whole animal studies? Whether the solvent contains any non-DMSO stabilizer?

Answer:
Our 10mM Ponatinib in DMSO solution is in pure DMSO and there is not other stabilizer added. You can use it for animal study. The vehicle we suggest for Ponatinib is: 30% PEG400/0.5% Tween80/5% Propylene glycol. It is a milky suspension used for oral gavage.

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