Imatinib (STI571)

Catalog No.S2475 Synonyms: Gleevec, Glivec, CGP057148B

For research use only.

Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.

Imatinib (STI571) Chemical Structure

CAS No. 152459-95-5

Selleck's Imatinib (STI571) has been cited by 251 publications

Purity & Quality Control

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Biological Activity

Description Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Targets
PDGFR [1]
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
In vitro

In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. [1] Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. [2] Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. [3] A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LAMA-84 NHz6[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMEezNFQh|ryP M4nlclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
EM-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzTWph{UUN3ME2wMlA5QDhizszN MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
MEG-01 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDUd5Q6UUN3ME2wMlA5QTJzIN88US=> M{L2c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
BV-173 NX\0Z2dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnlTWM2OD1yLkG4O|Qh|ryP M3Th[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
K-562 NH\aVJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrpfY5KSzVyPUCuNlI1OzJizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
CGTH-W-1 M1\uc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwM{izO|Qh|ryP NGDoWFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
ST486 M2L0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwNki1OEDPxE1? NUPwXI1sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
NCI-H1436 NEP3ZlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfEWllLUUN3ME2wMlk4QDBzIN88US=> MnrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
NOS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uwOGlEPTB;MT62OVM5OyEQvF2= M4P2R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
A498 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnexTWM2OD1{LkW3NlI{KM7:TR?= NGnuVYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
BE-13 MoD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjRNItKSzVyPUKuOlIyODZizszN NGnFS2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
SUP-T1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e5TWlEPTB;Mz64NlkxPyEQvF2= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
NCI-H1770 MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknmTWM2OD13LkW3NlYzKM7:TR?= M2DjXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
IMR-5 NUj3O3JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4qy[WlEPTB;Nj6yNlE1PyEQvF2= M3mwOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
LB2241-RCC MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fVTGlEPTB;OD6wO|M5PCEQvF2= Ml7VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
TGBC24TKB MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;lNmdUUUN3ME24MlM1ODV{IN88US=> M3XzRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
SCC-15 NUjBSJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn1NI9KSzVyPUGwMlc4QDhizszN Ml\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
BB49-HNC NETQe2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTF2LkOzN|Uh|ryP NX;qflBnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
ES7 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFizZYhKSzVyPUG0Mlc{PzlizszN MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
LB2518-MEL NEPUVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGxfYpsUUN3ME2xOk43ODl2IN88US=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
NCI-H510A MnfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTjbWhWUUN3ME2xO{4zPDR{IN88US=> M2LLUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
TE-441-T M3XSVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD0XnZXUUN3ME2xO{4zQDh4IN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
HH M4DJXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF5LkO5PVkh|ryP MkjPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
LC4-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXDTWM2OD1zOD6wOlUzKM7:TR?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
KARPAS-45 M2HORmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7tTWM2OD1zOD6xPFQ5KM7:TR?= M{\KOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
LB1047-RCC Ml23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPsVFZmUUN3ME2xPE41PDV{IN88US=> M1;zZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1OS9pPmPBUmdGWjxxYU6=
NKM-1 NHzKfGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTF7LkO1OVIh|ryP NXvYOVVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
SCLC-21H M3fwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\lTWM2OD1{MD6xNlQ3KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
RS4-11 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vMNGlEPTB;MkCuN|MxQCEQvF2= NX:4bZlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
ALL-PO NVn5eYczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmryTWM2OD1{MD64NVQ6KM7:TR?= MnfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
GDM-1 NXzEUVEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjsRWtKSzVyPUKyMlU6PDVizszN MnTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
DMS-79 M2rPWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJ2LkS5N|Qh|ryP NWH1TXluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
MPP-89 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonKTWM2OD1{NT62PFc1KM7:TR?= NHzrOVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
NB10 Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\0OIRKSzVyPUK2MlQ3QTlizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
LS-513 NV[wTmF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIriXVRKSzVyPUK2Mlg5PDdizszN NY\kc4V{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTRzLze+V2FPT0WUPD;hQi=>
L-540 NEW2c4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X2T2lEPTB;Mk[uPVE1OyEQvF2= MlqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
ES1 NVfFTldmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfaVpBKSzVyPUK3MlUzOSEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
NTERA-S-cl-D1 NF2zU2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzMPW13UUN3ME2zNE42ODl|IN88US=> MkjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
EW-1 M1fNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXBcJpYUUN3ME2zNk46PDV2IN88US=> NI\nblc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
Calu-6 NUjaVHhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTN|LkG4OVUh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
CTV-1 MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnu1TWM2OD1|Mz65O|g6KM7:TR?= NHnXVWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
YT NVXr[4JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vC[mlEPTB;M{iuOVIxQSEQvF2= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
TE-6 MoPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjQN2UyUUN3ME20NU4zPzl6IN88US=> NFXwcmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDFxJ{7TRW5ITVJ:L3G+
HT-144 MnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfITWM2OD12MT61OFg3KM7:TR?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFEwLz6VQV7HSXI9N2F-
EW-13 NXXwXoU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrPW|hKSzVyPUSyMlI4QTFizszN MnXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQyNyd-U1HOS2VTRC:jPh?=
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K562 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXu0PEBpenN? NHjTVYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkS3{txONg>? NX;ZUopIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3O|g4PjZpPkK1O|c5PzZ4PD;hQi=>
K562 M4\OfWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M2DBblczKGi{cx?= NVXtZ45oSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEKlcj3BZowh[W[2ZYKgO|IhcHK|IHL5JGNEUy16IHHzd4F6NCCLQ{WwQVAvOjkQvF2u MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF7NUGzOkc,OjZzOUWxN|Y9N2F-
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Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-STAT5 / STAT5 ; p-ZAP70 / ZAP70 / p-LAT / LAT ; p-STAT3 / STAT3 / p-STAT5 / STAT5 ; p-ZAP70 / ZAP70 / p-LAT / LAT 18981115
Immunofluorescence RelB ; Cortactin / F-actin ; RelB ; Cortactin / F-actin 20371728 20937825
Growth inhibition assay Cell viability 28435223
In vivo

Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. [5] In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. [6]

Protocol (from reference)

Kinase Assay:

[1]

  • PDGF receptor kinase activity:

    PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.

Cell Research:

[3]

  • Cell lines: BON-1 cells and NCI-H727 cells
  • Concentrations: ~100 μM
  • Incubation Time: 48 hours
  • Method:

    BON-1 cells and NCI-H727 cells are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 hours (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.

Solubility (25°C)

In vitro

DMSO 33 mg/mL
(66.85 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

2mg/mL

Chemical Information

Molecular Weight 493.6
Formula

C29H31N7O

CAS No. 152459-95-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05009927 Not yet recruiting Drug: Imatinib tablets Metastatic Gastrointestinal Stromal Tumor (GIST)|C-KIT Mutation|Advanced Gastrointestinal Stromal Tumor (GIST) Centre Leon Berard October 2021 Phase 2
NCT04933526 Not yet recruiting Drug: Flumatinib|Drug: Dasatinib Chronic Myeloid Leukemia in Chronic Phase Shenzhen Second People''s Hospital July 1 2021 Phase 4
NCT04903730 Recruiting Drug: AER-901 Solution for Nebulization|Drug: Placebo Pulmonary Arterial Hypertension Aerami Therapeutics May 24 2021 Phase 1
NCT04794088 Recruiting Drug: Imatinib Mesylate intravenous solution|Drug: Placebo ARDS|Acute Respiratory Distress Syndrome|Covid19|Endothelial Dysfunction|Pulmonary Edema Dr. Jurjan Aman|Simbec Orion|Exvastat Ltd.|KABS laboratories|VU University Medical Center March 14 2021 Phase 2
NCT03891901 Recruiting Drug: Imatinib|Drug: Isoniazid|Drug: Rifabutin Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) November 30 2020 Phase 2
NCT04326933 Not yet recruiting Drug: Tyrosine kinase Inhibitors (Imatinib & Nilotinib) Patients Diagnosed as Chronic Meyloid Leukemia Assiut University October 20 2020 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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:
Could you please advise whether it is a clear solution for compound dissolved in vehicle 2% DMSO+30% PEG 300+2% Tween 80+ddH2O?

Answer:
For S2475 Imatinib (STI571), it is soluble in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 2mg/ml. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm it in water bath at 45-50C. Then add PEG and Tween. After they mixed well, dilute with water.

Question 2:
What is the difference between S2475 (Imatinib) and S1026 (Imatinib Mesylate)? Are they water soluble?

Answer:
S2475 is free base of Imatinib while S1026 is a solt form of Imatinib. They have exactly the same biological activity but different solubility. S1026 can be dissolved in water, but S2475 is not soluble in water. S2475 can be dissolved in DMSO at up to 3mg/ml.

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