Ponatinib (AP24534)

For research use only.

Catalog No.S1490

141 publications

Ponatinib (AP24534) Chemical Structure

CAS No. 943319-70-8

Ponatinib (AP24534) 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.

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Selleck's Ponatinib (AP24534) has been cited by 141 publications

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Choose Selective Bcr-Abl Inhibitors

Biological Activity

Description Ponatinib (AP24534) 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)
0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell NHPqZo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rhZWlEPTB;MD6wNFAxODByM{W5JO69VQ>? MlvtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
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LAMA-84 NFj4c4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwMECwNVY2KM7:TR?= NHvaSIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
CGTH-W-1 M3\IZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn4TWM2OD1yLkCwNVY6KM7:TR?= NEXkbXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
KASUMI-1 NHjyU|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7CXGxKSzVyPUCuNFAzOTdizszN Mn7tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
BE-13 NYThNHNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1n0fmlEPTB;MD6wNFI2QSEQvF2= NUHuWWhZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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NKM-1 NIDHS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\LTmlEPTB;MD6wNFY2PSEQvF2= NGO1PFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
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Daudi NHnDUpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwMEK1N|ch|ryP Mn\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
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DOHH-2 MnS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnL0TWM2OD1yLkC0PFA{KM7:TR?= MnfTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
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SU-DHL-1 M2HLV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzO[m1KSzVyPUCuNFY{PzlizszN MoHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
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LB996-RCC MlzWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Pyb2lEPTB;Mj6xN|gyPyEQvF2= M2TPNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
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NCI-H1792 M2fxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjOZVBOUUN3ME2yMlU3QDJ4IN88US=> NH:2bWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
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COLO-679 MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTiOWlJUUN3ME2yMlU5PjB3IN88US=> M1rlTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
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Ramos-2G6-4C10 MlzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2WyR2lEPTB;Mj62OFgxPyEQvF2= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
HCT-15 MnfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M176ZmlEPTB;Mj62PFc6OiEQvF2= NXXaTZljRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
MDA-MB-157 M4SwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X0PWlEPTB;Mj63NFc1PyEQvF2= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
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MKN45 NELmWJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTJwN{OzOlYh|ryP M3XQWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
DMS-273 NIroPZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\pNmlEPTB;Mj63OVY{OiEQvF2= MoXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
C8166 MkfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NICxb4NKSzVyPUKuO|g2OTNizszN MoD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
Calu-3 NI\qUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrHTWM2OD1{Lke4PVY6KM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
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BFTC-905 NF;2OlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJwOUCxPVEh|ryP NWX2UGlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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MS-1 M4PFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f3dGlEPTB;Mj65Olc3QSEQvF2= M4n3TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
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KYSE-70 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTNwMEi4PFIh|ryP MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
KYSE-510 Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvuTWM2OD1|LkGwPVk2KM7:TR?= NFnBSmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LN-405 MlPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvFfpZQUUN3ME2zMlE{PTF6IN88US=> NVfvZmVuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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M14 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTR|LkOxPFkh|ryP MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
NCI-H1623 NIDsdldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHPWXE4UUN3ME20N{41PjRizszN NXHhbohrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
KNS-81-FD NYKybJE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Hq[GlEPTB;NEOuO|YzKM7:TR?= M3fnR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
TGBC1TKB MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHafplKSzVyPUSzMlkxQTlizszN MlrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
RERF-LC-MS MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInwWmVKSzVyPUSzMlkzQDFizszN M4TrV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
PC-3 M1\rV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPCTG9KSzVyPUS0MlQ{PDdizszN MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
HuP-T4 NGiyNppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3wTWM2OD12ND60OFc1KM7:TR?= NGm3ZWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
NCI-H510A MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jzfmlEPTB;NESuO|A5KM7:TR?= M2OwUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
LB2518-MEL NEPWTIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmC5TWM2OD12ND63PVM4KM7:TR?= M1\1dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
TE-5 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTVWYlKSzVyPUS1Mlk2QDFizszN NXHCOoFnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
EW-24 NHjWWZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\oO2lEPTB;NE[uNVczOyEQvF2= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
LB647-SCLC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR4LkKxOVUh|ryP NFPKfJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
NCI-H524 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX33e2lDUUN3ME20Ok44OTh3IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
EW-11 MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPWTVQ1UUN3ME20Ok46Ozd|IN88US=> NHPteFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
KALS-1 M1T4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPpWYdKSzVyPUS3MlIxPjZizszN M{TER|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
BT-474 Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfX[lcyUUN3ME20O{41OjF4IN88US=> NYq0VnVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
SK-N-AS NGDabXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfJNmRCUUN3ME20O{45QDhizszN MofsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
HCC2157 NVHsUYVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7MTWM2OD12OD6wO|Yh|ryP Mki0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
HCC1954 Ml;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\lTWM2OD12OD6xO|A1KM7:TR?= NXr4OGE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
FADU M4\wXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXXfY1KSzVyPUS4MlMxOzFizszN MnSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
S-117 M3riS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTtS3RKSzVyPUS4MlM5OTVizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
LS-1034 NXrVVW5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTR6LkewOlch|ryP MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
CAMA-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR7LkW1OFMh|ryP NFrNfVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LU-134-A NFTTVm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nlTGlEPTB;NEmuPFA5PSEQvF2= M4H4UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
NCI-H1838 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S2TmlEPTB;NEmuPFA5PyEQvF2= MlnnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pSrc / Src / pPlcg / Plcg / pStat5 / Stat5 ; 

PubMed: 22781593     


In (B) inhibition of Src, Plcg and Stat5 was seen in MLNAF cell lines treated with Ponatinib; ZNF112 expresses ZMYM2–FGFR1, CEP2A and CEP5A cells express CEP110–FGFR1 and BBC2 expresses BCR–FGFR1.

pFGFR1(pY20) / FGFR1; 

PubMed: 22781593     


Western blot analysis, using various antibodies specific for downstream targets of FGFR1, demonstrates that Ponatinib inhibits the activation of Plcg and Src as a result of inhibiting the FGFR1 fusion kinase in human KG1 cells. 

cleaved caspase-3 / cleaved caspase-7 / BAX / Bcl-2; 

PubMed: 30959969     


Western blot analysis of cleaved caspase-3, cleaved caspase-7, Bax, Bcl-2, and β-Tubulin (control) in treated cells.

p-Rb(S807/811) / Rb / CDK4 / CDK6 / Cyclin D1 / CDK2 / Cyclin E1; 

PubMed: 30959969     


Western blot analysis of Rb/p-Rb, CDK4, CDK6, Cyclin D1, CDK2, Cyclin E1, and β-Tubulin (control) in the SK-Hep-1 and SNU-423 cells treated with ponatinib. 

RAD51; 

PubMed: 30959969     


The effect of ponatinib on the concentration of Rad51 in SK-Hep-1 and SNU-423 cells.

p-MEK / MEK / p-ERK / ERK; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of Mek and Erk. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

c-Jun / p-JNK(T183/Y185) / JNK; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of JNK and c-Jun. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

p-p38 MAPK / p38 MAPK; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of p38. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

p-JAK2 / JAK2 / p-STAT3 / STAT3; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of Jak2, and Stat3. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

PI3K p85 / p-PI3K / p-PDK1 / PDK1 / p-mTOR / mTOR; 

PubMed: 30959969     


Effects of ponatinib on the protein concentration and phosphorylation of PI 3-kinase, PDK1, Akt, and mTOR in HCC cells. 

p-PDGFRα / PDGFRα; 

PubMed: 24472312     


Ponatinib inhibited phosphorylation of PDGFRα in a concentration-dependent manner. EOL-1 and BaF3-WT or -T674I FIP1L1-PDGFRα cells were exposed to escalating concentrations of ponatinib for 24 h.

PARP / Caspase-3 / Active Caspase-3; 

PubMed: 24472312     


The concentration- (for 24 h) and time-dependent (1 nM for EOL-1, 300 nM for BaF3-WT and -T674I FIP1L1-PDGFRα cells) cleavage of PARP and caspase-3 triggered by ponatinib was analyzed by immunoblotting.

AIF / Cyto C ; 

PubMed: 24472312     


Ponatinib elicited release of AIF and cytochrome c into the cytosol. Cells were treated with 1 nM ponatinib for the indicated durations and the cytosolic fraction was extracted with digitonin buffer. Levels of AIF and Cytochrome c (Cyto c) were detected by immunoblotting.

Mcl-1 / Survivin / Bcl-Xl / XIAP / Bax / Bcl-2 / Bim; 

PubMed: 24472312     


Immunoblotting of apoptosis-related proteins in CEL cells after treatment for 24 h.

β-catenin ; 

PubMed: 24472312     


Ponatinib concentration-dependently lowered β-catenin. EOL-1 cells were incubated with ponatinib for 24 h, and cytoplasmic and nuclear extracts were determined by immunoblotting.

β-catenin; 

PubMed: 24472312     


Analysis of β-catenin localization. EOL-1 cells were pretreated with 1 nM ponatinib for 24 h, immunofluorescence analysis was performed with anti-β-catenin. Nuclei were stained with 4,6-diamidino-2-phenylindole (DAPI). 

ABL; 

PubMed: 19878872     


In vitro [γ-32P]-ATP autophosphorylation of full-length (A) ABL or (B) ABLT315I kinase treated with AP24534, imatinib, nilotinib, or dasatinib. After incubation of tyrosine-dephosphorylated enzyme with the indicated inhibitor in the presence of [γ-32P]-ATP and separation by SDS-PAGE, signal intensity was measured by autoradiography.

22781593 30959969 24472312 19878872
Growth inhibition assay
Cell viability; 

PubMed: 30174789     


(A) Effect of Ponatinib on basal viability of HUVECs. The cells were treated with Ponatinib at indicated concentrations or 0.1% DMSO (vehicle control) for 24 h.

30174789
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]

Protocol

Kinase Assay:[1]
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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:[2]
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  • 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
    (Only for Reference)
Animal Research:[1]
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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 30 mg/mL (56.33 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
30mg/mL

* 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 532.56
Formula

C29H27F3N6O

CAS No. 943319-70-8
Storage powder
in solvent
Synonyms N/A
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

In vivo Formulation Calculator (Clear solution)

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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)

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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 )

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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

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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
NCT04554459 Not yet recruiting Drug: Ponatinib 15 MG Oral Tablet Acute Lymphoblastic Leukemia Adult|Ph+ ALL|Newly Diagnosed Institute of Hematology and Blood Transfusion Czech Republic|CZECRIN - Czech Clinical Research Infrastructure Network October 30 2020 Phase 2
NCT04160546 Recruiting Drug: Ponatinib 15 MG|Drug: Acetylsalicylic acid 100 MG Chronic Myeloid Leukemia Chronic Phase Fundacion CRIS de Investigación para Vencer el Cáncer|Incyte Biosciences UK|Apices Soluciones S.L. January 17 2020 Phase 2
NCT03934372 Recruiting Drug: Ponatinib Acute Myeloid Leukemia|Accelerated Phase Chronic Myeloid Leukemia|Blast Phase Chronic Myeloid Leukemia|Chronic Phase Chronic Myeloid Leukemia|Acute Lymphoblastic Leukemia|Acute Lymphocytic Leukemia|Leukemia|Lymphoma|Solid Tumors Incyte Biosciences International Sàrl|Incyte Corporation January 29 2020 Phase 1|Phase 2
NCT04070443 Recruiting Drug: Ponatinib|Drug: Imatinib Philadelphia Chromosome Positive CML|BCR-ABL Positive Chronic Myelogenous Leukemia Centre Leon Berard November 13 2019 Phase 2
NCT03895671 Recruiting Drug: Ponatinib|Drug: Azacitidine CHRONIC MYELOGENOUS LEUKAEMIA IN ACCELERATED PHASE|CHRONIC MYELOGENOUS LEUKAEMIA IN MYELOID BLAST CRISIS Versailles Hospital June 19 2019 Phase 2

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.

  • * Indicates a Required Field

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID