Ponatinib (AP24534)

For research use only. Not for use in humans.

目录号：S1490 中文名称：帕纳替尼

CAS No. 943319-70-8

Ponatinib (AP24534)是一种新型有效的多靶点抑制剂，在无细胞试验中作用于Abl，PDGFRα，VEGFR2，FGFR1和Src，IC50分别为0.37 nM，1.1 nM，1.5 nM，2.2 nM和5.4 nM。Ponatinib (AP24534)可抑制自噬。

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10mM (1mL in DMSO)	RMB 819.31	现货
10mg	RMB 903.01	现货
50mg	RMB 3034.48	现货
200mg	RMB 7959.08	现货
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客户使用Selleck生产的Ponatinib (AP24534)发表文献138篇：

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Gut, 2016, 10.1136/gutjnl-2015-310382

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Blood, 2016, 28;127(17):2131-43

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Hepatology, 2016, 64(2):488-500

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J Thorac Oncol, 2016, 11(8):1273-1281

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Mol Cell Proteomics, 2016, 15(3):1139-50

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产品安全说明书

Bcr-Abl抑制剂选择性比较

生物活性

产品描述

靶点

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)	点击更多
0.37 nM	1.1 nM	1.5 nM	2.2 nM	5.4 nM	点击更多

体外研究

Ponatinib是有效的可用于口服的多靶点激酶抑制剂，作用于野生型细胞,及T315I 突变细胞IC50分别为1.2和8.8nM。^[1] Ponatinib抑制Ba/F3衍生细胞系的增殖。^[2] Ponatinib作用于表达野生型或T315I突变型BCR-ABL的CML细胞系，有效抑制BCR-ABL调节的信号。Ponatinib阻断在细胞瘤筛选时产生抗性突变。^[3] Ponatinib也抑制VEGFR和FGFR家族激酶，在体外抑制FLT3, KIT, FGFR1,和PDGFRa激酶活性时IC50分别为13, 13, 2, 和1 nM.^[4]Ponatinib抑制全部4种RTKs磷酸化，存在剂量依赖性，IC50值为0.3到20 nM。然而，Ponatinib抑制表达野生型FLT3的RS4;11细胞时IC50>100 nM。

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
EoL-1-cell	NVXqXmVQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXrlToJlUUN3ME2wMlAxODByMECzOVkh\|ryP	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
MV-4-11	NEjuVJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXHDRlJkUUN3ME2wMlAxODB7NU[g{txO	NYTrbXp5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
MEG-01	M2nD[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFraUFJKSzVyPUCuNFAxOTJ6IN88US=>	MmrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
LAMA-84	M2PnXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3f2RWlEPTB;MD6wNFAyPjVizszN	NYHTOGg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
CGTH-W-1	NHjZclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2D5b2lEPTB;MD6wNFE3QSEQvF2=	NEPZcJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
KASUMI-1	M3WyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXTDSJVKUUN3ME2wMlAxOjF5IN88US=>	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
BE-13	NH3HZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFr2eYlKSzVyPUCuNFAzPTlizszN	NHjoN\|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
CTV-1	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWq5RoE6UUN3ME2wMlAxPTJzIN88US=>	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
NKM-1	NWDx[mVNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWXUXXlZUUN3ME2wMlAxPjV3IN88US=>	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
MONO-MAC-6	NVHPZo5NT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXPJR\|UxRTBwMEC4N\|ch\|ryP	NWjPN\|RJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
A204	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVLJR\|UxRTBwMEGyNVgh\|ryP	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
GDM-1	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWS0VFR5UUN3ME2wMlAyQDN\|IN88US=>	NYHlNHd1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
AN3-CA	NF7wOYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NX[xeGh3UUN3ME2wMlAyQDd\|IN88US=>	NWXUTndsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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IA-LM	NWO2XGZIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXPJR\|UxRTFwNEC5NVQh\|ryP	MlnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
MN-60	MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2e4NWlEPTB;MT60N\|EyPCEQvF2=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
SIMA	M4fpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWnJR\|UxRTFwNEi2PFch\|ryP	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
NCI-H1770	NHzrNIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NH24W2xKSzVyPUGuOVIxPTRizszN	M{HDPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
ONS-76	Ml7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2PIZWlEPTB;MT61NlMyOSEQvF2=	NVWwXJdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
LB771-HNC	MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mk\sTWM2OD1zLkWzPVA3KM7:TR?=	M1ywPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
SW48	MlzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXzZXJU3UUN3ME2xMlU1OjR\|IN88US=>	MkLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
KYSE-140	M{j2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MorlTWM2OD1zLkW1O\|QyKM7:TR?=	NFjzXGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
SW626	M2DjfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkDzTWM2OD1zLkW4NVYh\|ryP	NEXsVZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
MC-CAR	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHXCZ\|RKSzVyPUGuOVg3PjNizszN	M2\DUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
D-336MG	NY\Jc2Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn;TTWM2OD1zLk[yPVQh\|ryP	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
SK-MEL-3	NH7yW4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnXGTWM2OD1zLk[zPVAzKM7:TR?=	NGX5cmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
MHH-PREB-1	M3vlcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV;JR\|UxRTFwNkS0O\|Mh\|ryP	NIS1cmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
Calu-1	M3rxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXLJR\|UxRTFwNkWzPFYh\|ryP	NG\1Rno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
HCC1806	NEK0N4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVTJR\|UxRTFwNk[2NVEh\|ryP	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
A101D	M{LEZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXnJR\|UxRTFwNk[3PFEh\|ryP	M{DJVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
A704	M1nneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXXzdWIzUUN3ME2xMlY5OzFzIN88US=>	NIXt[o89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LB831-BLC	NYP6O21lT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXvwb3dOUUN3ME2xMlY6QDV2IN88US=>	NVLuPY9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
RL95-2	M{C3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGLHd\|RKSzVyPUGuO\|E1PjNizszN	MkHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
RPMI-2650	M4\yVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoK1TWM2OD1zLkeyO\|E6KM7:TR?=	M3fSOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
NH-12	NX7jfldsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXy5U451UUN3ME2xMlc{PDJ5IN88US=>	NHjzV\|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
AGS	M4W3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkXqTWM2OD1zLke2N\|U5KM7:TR?=	M{fHS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
NEC8	MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnfMTWM2OD1zLke4PVk2KM7:TR?=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
NCI-H2009	M{Cybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGeyO5ZKSzVyPUGuO\|k4OjFizszN	M3O4UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
A498	MoPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{OyfGlEPTB;MT64NVI5OiEQvF2=	M33nUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
NCI-H810	MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF7zNoZKSzVyPUGuPFE3ODZizszN	M1jRWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
SK-NEP-1	M1LFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWPTSm51UUN3ME2xMlg{PzZ5IN88US=>	M3;3flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
D-542MG	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{nFZWlEPTB;MT64OVg2OSEQvF2=	MmrWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
KNS-42	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUHJR\|UxRTFwOE[yOlYh\|ryP	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
NCI-H2452	Mm\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NULHUnFXUUN3ME2xMlg6ODd2IN88US=>	M{ezUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
SK-MEL-2	NEHTXZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlLJTWM2OD1zLkmwNlcyKM7:TR?=	MmnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
OVCAR-5	NWHKcpNJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF:4eYdKSzVyPUGuPVA3PzVizszN	NHLvc2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
SNG-M	NHnLOGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUHJR\|UxRTFwOUW4OVgh\|ryP	M3TvdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
A673	M2X3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWnRbIx{UUN3ME2xMlk4PTF4IN88US=>	NFezZXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
L-428	NEjoeItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnvLTWM2OD1zLkm5NVc6KM7:TR?=	Mn;lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
KM-H2	NEDjeGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2PCTGlEPTB;Mj6wNVA6KM7:TR?=	NX3oNHU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
MC-IXC	NGiy[pNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEPHOW5KSzVyPUKuNFIzPzNizszN	NG\MU\|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
COLO-678	NGruVmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnTVTWM2OD1{LkC0NlA4KM7:TR?=	NIfJWZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
MEL-JUSO	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXXnNHdmUUN3ME2yMlA4QDVzIN88US=>	NV\Pdo92RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
HCC38	M2G3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVPJR\|UxRTJwMEi0N\|Mh\|ryP	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
UACC-62	MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NX3yV2Q5UUN3ME2yMlA5QDV3IN88US=>	M2\OVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
OAW-42	M120c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoTCTWM2OD1{LkC5O\|EyKM7:TR?=	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
LB996-RCC	NWi2ZlNjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnvPTWM2OD1{LkGzPFE4KM7:TR?=	NWft[YVYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
COR-L105	NEe1UXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYjJR\|UxRTJwMU[zO\|Mh\|ryP	M1yxb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
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COLO-829	NUjicodQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2jySGlEPTB;ND63O\|A1OyEQvF2=	NVnFS5JZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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HAL-01	NUTTS3pWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4HUc2lEPTB;NT6xOFY1PSEQvF2=	NGHqXFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
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ChaGo-K-1	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVvJR\|UxRTVwM{WxNFch\|ryP	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
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NB69	MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEXjVGZKSzVyPUWuN\|k3OzFizszN	M{i1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
NCI-H1882	M4jtZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHPVd4JKSzVyPUWuOFM{PjRizszN	NV6zclZ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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CAL-51	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVrUfGxOUUN3ME21MlYzQDV\|IN88US=>	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
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GCT	M1e5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4HxRmlEPTB;NT63OVkzQSEQvF2=	NWTzTZV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
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LB2518-MEL	MkO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MljZTWM2OD12ND63PVM4KM7:TR?=	NGrQW2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
TE-5	M3PsRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2TXfmlEPTB;NEWuPVU5OSEQvF2=	MkjDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
EW-24	MmnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2LqOmlEPTB;NE[uNVczOyEQvF2=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
LB647-SCLC	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHjTcmVKSzVyPUS2MlIyPTVizszN	M2K0UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
NCI-H524	MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVHTdIFNUUN3ME20Ok44OTh3IN88US=>	NIrGOIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
EW-11	NHzyZlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVH2eItnUUN3ME20Ok46Ozd\|IN88US=>	M2nielxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
KALS-1	NYWxUIxOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3nLeGlEPTB;NEeuNlA3PiEQvF2=	MoPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
BT-474	M1ezPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnnyTWM2OD12Nz60NlE3KM7:TR?=	M2XhcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
SK-N-AS	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkXPTWM2OD12Nz64PFgh\|ryP	M2OyV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
HCC2157	M4K2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVPvSGY2UUN3ME20PE4xPzZizszN	MkT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
HCC1954	NFX5VnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlzBTWM2OD12OD6xO\|A1KM7:TR?=	MnTxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh\|Nz:nQnNCVkeHUkyvZV4>
FADU	NWLhWIJJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWnrVIlWUUN3ME20PE4{ODNzIN88US=>	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
S-117	Ml:wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF3hNWtKSzVyPUS4MlM5OTVizszN	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
LS-1034	MoDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1W0c2lEPTB;NEiuO\|A3PyEQvF2=	M2rNSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK\|5USU6JRWK8M4E,
CAMA-1	NGP5bIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MorDTWM2OD12OT61OVQ{KM7:TR?=	NGq1cYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LU-134-A	NGXRNVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mnr2TWM2OD12OT64NFg2KM7:TR?=	NX;YXHpJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
NCI-H1838	M4rE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mli4TWM2OD12OT64NFg4KM7:TR?=	NGn4cJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pSrc / Src / pPlcg / Plcg / pStat5 / Stat5 ; PubMed: 22781593 Leukemia 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 Leukemia 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 Molecules 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 Molecules 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 Molecules 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 Molecules 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 Molecules 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 Molecules 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 Molecules 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 Molecules 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 Mol Cancer 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 Mol Cancer 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 Mol Cancer 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 Mol Cancer Immunoblotting of apoptosis-related proteins in CEL cells after treatment for 24 h. β-catenin ; PubMed: 24472312 Mol Cancer 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 Mol Cancer 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 Cancer Cell 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 Oncotarget (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

体内研究

Ponatinib抑制取自FLT3-ITD阳性AML病人的原代白血病细胞，而不抑制表达阴性FLT3的AML病人的白血病细胞。^[3]

激酶实验：^[1]	- 合并激酶实验: 通过同质时间分辨荧光共振能量转移法(TR-FRET)，使用纯化的人类野生型ABL激酶，T315I突变型ABL激酶，及生物素化的磷酸激酶底物肽: 生物素-EKKMAAEAIYAAPFAK-NH2，测定野生型ABL和T315I突变型ABL活性的抑制激酶反应在全LANCE激酶buffer (LKB)中进行，LKB包括20 mM NaHEPES（pH 为7.4）, 0.1 mg ⁄ mL BSA, 1 mM ATP, 10 mM MgCl₂, 及0.41 mM DTT，在提前用1% BSA（溶于PBS）包被的96孔板上4^oC下过夜。用于激酶反应，Ponatinib稀释物和野生型ABL, T315I突变型ABL (40 pM), 及底物肽(50 nM), 在室温下温育1小时（T315I突变型ABL）或2小时（野生型ABL）。加入15 nM 抑制剂, 6 nM 铕标记的磷酸酪氨酸抗体（磷酸化位点在第66为酪氨酸上），及60 nM 别藻蓝素标记的链酶亲和素，终止反应。实验板在室温下黑暗温育20分钟，使用Wallac Victor2V读数器读取615和665nm处的荧光值。在孔中数据平均值中插入抑制剂的3倍连续稀释液，再读取665nm处荧光值，计算IC50值。
细胞实验：^[1]	- 合并 Cell lines: Ba ⁄ F3细胞 Concentrations: 0-625 nM, 和0-10 µM Incubation Time: 72小时 Method: Ba/F3细胞系按每孔4×10³个细胞分布在96孔板上(4×10³)，和梯度浓度Ponatinib温育72小时。Ponatinib浓度范围为: 0-625 nM 作用于表达BCR-ABL细胞，0-10 µM 用于测定BCR-ABL阴性细胞。使用MTS实验测定细胞增殖，取三次平行实验平均值测定IC50值。 (Only for Reference)
动物实验：^[3]	- 合并 Animal Models: 皮下植入MV4-11细胞移植瘤(1×10⁷，50%基质胶中) 的雌性CB.17 SCID鼠 Dosages: 每天处理一次，持续4周 Administration: 口服饲喂处理 (Only for Reference)

参考文献

- 合并

溶解度 (25°C)

体外	DMSO	30 mg/mL (56.33 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 1% CMC Na	30mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Ponatinib (AP24534) SDF

分子量	532.56
化学式	C₂₉H₂₇F₃N₆O
CAS号	943319-70-8
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

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

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
Is the pre-solubilized inhibitor suitable for in vivo whole animal studies? Whether the solvent contains any non-DMSO stabilizer?
回答：
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.

Bcr-Abl Signaling Pathway Map

Bcr-Abl Inhibitors with Unique Features

选择性强的Bcr-Abl抑制剂

Nilotinib (AMN-107) : Bcr-Abl-selective, IC50<30 nM.
活性最高的Bcr-Abl抑制剂

GZD824 : Bcr-Abl(WT), IC50=0.34 nM; Bcr-Abl(T315I), IC50=0.68 nM.
FDA批准的Bcr-Abl抑制剂

Dasatinib : Approved by FDA for CML and Ph+ ALL.
最新的Bcr-Abl抑制剂

GZD824 : Orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

研究领域

产品类型

定制您的化合物库

Ponatinib (AP24534)

客户使用Selleck生产的Ponatinib (AP24534)发表文献138篇：

产品安全说明书

Bcr-Abl抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Ponatinib (AP24534) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技术支持

常见问题及建议解决方法

Bcr-Abl Signaling Pathway Map

Bcr-Abl Inhibitors with Unique Features

相关Bcr-Abl产品