Imatinib (STI571)

Catalog No.S2475 Synonyms: CGP057148B, ST-1571

Imatinib (STI571) Chemical Structure

Molecular Weight(MW): 493.6

Imatinib (STI571) 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.

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Cited by 89 Publications

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Imatinib (STI571) 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.
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 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7pd2JoUUN3ME2wMlA4OzB2IN88US=> MVnTRW5ITVJ?
EM-2 NEGzTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fsRWlEPTB;MD6wPFg5KM7:TR?= M2TGNnNCVkeHUh?=
MEG-01 M1q2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTBwMEi5NlEh|ryP M3PrcXNCVkeHUh?=
BV-173 MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMUi3OEDPxE1? MWrTRW5ITVJ?
K-562 NY\tXmZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLHTWM2OD1yLkKyOFMzKM7:TR?= NXG4N5RKW0GQR1XS
CGTH-W-1 Mn7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwM{izO|Qh|ryP NYnsZXE5W0GQR1XS
ST486 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noZmlEPTB;MD62PFU1KM7:TR?= NGL3SXRUSU6JRWK=
NCI-H1436 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TDdmlEPTB;MD65O|gxOSEQvF2= Ml7XV2FPT0WU
NOS-1 NUXZb2VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDUS3dGUUN3ME2xMlY2Ozh|IN88US=> MXTTRW5ITVJ?
A498 NXG1doE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfVcJljUUN3ME2yMlU4OjJ|IN88US=> NWfOfFdMW0GQR1XS
BE-13 M3Xyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJwNkKxNFYh|ryP NIX1RlFUSU6JRWK=
SUP-T1 M3ryemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:3TWM2OD1|LkiyPVA4KM7:TR?= NGnuN2JUSU6JRWK=
NCI-H1770 NUfJU4FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofETWM2OD13LkW3NlYzKM7:TR?= MXHTRW5ITVJ?
IMR-5 NWLrW2M1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXkWG9qUUN3ME22MlIzOTR5IN88US=> NWj1eJlCW0GQR1XS
LB2241-RCC NGXIb3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DXOWlEPTB;OD6wO|M5PCEQvF2= MYjTRW5ITVJ?
TGBC24TKB NVjaR3M1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrtWIdKSzVyPUiuN|QxPTJizszN M2jhR3NCVkeHUh?=
SCC-15 NEDnUWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzrTYVnUUN3ME2xNE44Pzh6IN88US=> MYXTRW5ITVJ?
BB49-HNC MlfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF2LkOzN|Uh|ryP MV7TRW5ITVJ?
ES7 NFHtc5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDmW4hKSzVyPUG0Mlc{PzlizszN MVTTRW5ITVJ?
LB2518-MEL MlzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHIXYR5UUN3ME2xOk43ODl2IN88US=> NELJdYpUSU6JRWK=
NCI-H510A MkG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m2T2lEPTB;MUeuNlQ1OiEQvF2= NX[0UmpqW0GQR1XS
TE-441-T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm5TWM2OD1zNz6yPFg3KM7:TR?= NIDYUWlUSU6JRWK=
HH MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nob2lEPTB;MUeuN|k6QSEQvF2= NGrWUYFUSU6JRWK=
LC4-1 MlTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\yTWM2OD1zOD6wOlUzKM7:TR?= NIC1cGRUSU6JRWK=
KARPAS-45 NV\OdlZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDk[4h{UUN3ME2xPE4yQDR6IN88US=> NUi0Uo9CW0GQR1XS
LB1047-RCC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvUTWM2OD1zOD60OFUzKM7:TR?= MWXTRW5ITVJ?
NKM-1 MorjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP5TWM2OD1zOT6zOVUzKM7:TR?= NVv6SYJXW0GQR1XS
SCLC-21H MkjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHG4cWFKSzVyPUKwMlEzPDZizszN MVXTRW5ITVJ?
RS4-11 NHzieWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[yTWM2OD1{MD6zN|A5KM7:TR?= Mnq2V2FPT0WU
ALL-PO NV[zUZVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvnTWM2OD1{MD64NVQ6KM7:TR?= M3jmcHNCVkeHUh?=
GDM-1 MnXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojTTWM2OD1{Mj61PVQ2KM7:TR?= M1HDfXNCVkeHUh?=
DMS-79 NE\rOFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED3OFFKSzVyPUK0MlQ6OzRizszN Mof6V2FPT0WU
MPP-89 Mkm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqyTWM2OD1{NT62PFc1KM7:TR?= M1HHS3NCVkeHUh?=
NB10 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWKxbnlsUUN3ME2yOk41Pjl7IN88US=> NWi4Z4NEW0GQR1XS
LS-513 M2L5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv3TWM2OD1{Nj64PFQ4KM7:TR?= Mo\vV2FPT0WU
L-540 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHUTVNKSzVyPUK2MlkyPDNizszN M37tTHNCVkeHUh?=
ES1 NWDDb5hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr6cJRKSzVyPUK3MlUzOSEQvF2= Moj6V2FPT0WU
NTERA-S-cl-D1 M1[zZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXTTWM2OD1|MD61NFk{KM7:TR?= MWTTRW5ITVJ?
EW-1 NEHVb3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDjUoJKSzVyPUOyMlk1PTRizszN MmPUV2FPT0WU
Calu-6 NVnqfoxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjyTWM2OD1|Mz6xPFU2KM7:TR?= NILaXlNUSU6JRWK=
CTV-1 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HFVmlEPTB;M{OuPVc5QSEQvF2= NFrBeFFUSU6JRWK=
YT NU[wVFhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXsTWM2OD1|OD61NlA6KM7:TR?= NF7YT2tUSU6JRWK=
TE-6 NVH4blJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTiR4pWUUN3ME20NU4zPzl6IN88US=> NEewT2FUSU6JRWK=
HT-144 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TZT2lEPTB;NEGuOVQ5PiEQvF2= MlH4V2FPT0WU
EW-13 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\DPYN3UUN3ME20Nk4zPzlzIN88US=> NFTMVItUSU6JRWK=
KALS-1 NXrpVVZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTR|LkGzNlkh|ryP Mnf1V2FPT0WU
MOLT-16 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HXeGlEPTB;NEWuNFc2OiEQvF2= M3XNdHNCVkeHUh?=
D-336MG MoPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7IXoM5UUN3ME20OU46PTl7IN88US=> M{DXPXNCVkeHUh?=
TE-11 M3nhOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\lTWM2OD12Nj62OVMh|ryP M4rYcHNCVkeHUh?=
EB2 MkW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXCWpY5UUN3ME20Ok43QTlizszN NF7scY9USU6JRWK=
SK-N-DZ MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPKTWM2OD12OD6wPVYyKM7:TR?= NHn2enBUSU6JRWK=
SW684 MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jOfWlEPTB;NEiuNlY6PSEQvF2= NYTnS3NpW0GQR1XS
EW-18 M2\BbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPq[oQ1UUN3ME20PE41Ozl3IN88US=> NHThcItUSU6JRWK=
RL95-2 M1zz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLFV|B7UUN3ME21NE4xPzFizszN NU[yfFhnW0GQR1XS
CHP-126 NIXPeGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfjPVJzUUN3ME21NE45QTB3IN88US=> NELzdG9USU6JRWK=
NCI-H1395 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHWTWM2OD13MT63PFM2KM7:TR?= MVnTRW5ITVJ?
TE-15 NVP4Vpk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\qTGpKUUN3ME21Nk4zPTV4IN88US=> MVHTRW5ITVJ?
ES4 NWriW|lGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H2TGlEPTB;NUKuPVc4PSEQvF2= MVjTRW5ITVJ?
TE-1 M13YZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LLS2lEPTB;NUOuPVQ2PSEQvF2= M4PsN3NCVkeHUh?=
SIMA NHe4bpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XjXGlEPTB;NUeuN|MyOSEQvF2= NUfyenpxW0GQR1XS
LB647-SCLC M2j4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTZ2LkGxPFgh|ryP MojOV2FPT0WU
KY821 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnzW|FNUUN3ME22OE4zPTV{IN88US=> NXPGXGRuW0GQR1XS
LC-2-ad Mlm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1iyO2lEPTB;NkWuO|YxOSEQvF2= M2PVb3NCVkeHUh?=
KP-N-RT-BM-1 NG\VVZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PNTmlEPTB;Nk[uOlM3PiEQvF2= M3HF[XNCVkeHUh?=
SW872 M3jUV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUP3eZFmUUN3ME22O{41Ozh{IN88US=> MlTvV2FPT0WU
ES5 M1PYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzDZlVKSzVyPU[3MlY6PjhizszN M1PMUHNCVkeHUh?=
SK-NEP-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDCcW1KSzVyPU[4MlM5ODNizszN M1LwZnNCVkeHUh?=
RPMI-6666 NWL2R|QzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXYOIpKSzVyPUexMlA{OiEQvF2= M1:0ZnNCVkeHUh?=
UACC-812 NXPMWnJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT5TWM2OD15MT6xOlA6KM7:TR?= MXvTRW5ITVJ?
COLO-829 M3Hscmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfON4pKSzVyPUeyMlY6QDdizszN NXrNV5l3W0GQR1XS
KP-N-YS NYLmd2M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOwT29qUUN3ME23Nk44OTN7IN88US=> M4jRVHNCVkeHUh?=
GI-1 M{LGRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn2XZNKSzVyPUezMlI5PjhizszN NULwPFZpW0GQR1XS
ETK-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\F[2lEPTB;N{OuOFk{OiEQvF2= NWnqWY9OW0GQR1XS
LXF-289 Ml22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HrWGlEPTB;N{OuO|I6KM7:TR?= NVTac|A{W0GQR1XS
CAS-1 MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTd|Lki4OVch|ryP NGPCSJhUSU6JRWK=
EW-22 M3P1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnt[Zo{UUN3ME23OE44OTF3IN88US=> NUPVSYVCW0GQR1XS
NCI-H2196 M2\wc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXYOFNCUUN3ME23OU43Ozd7IN88US=> NWDofopuW0GQR1XS
EoL-1-cell M2my[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvwTWM2OD16MT62PVY{KM7:TR?= M{fWXXNCVkeHUh?=
D-247MG NV;lbIE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHtTWM2OD16Mj6wNlQ5KM7:TR?= M3;4WnNCVkeHUh?=
Becker MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn0TW9KSzVyPUiyMlM1QDFizszN NE\i[YJUSU6JRWK=
IST-MEL1 NEfOVZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXFbnQxUUN3ME24Nk4{PDh{IN88US=> M3i0UXNCVkeHUh?=
MDA-MB-134-VI NIXIRnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\afmNKSzVyPUiyMlU6QTZizszN MVfTRW5ITVJ?
NCI-H1092 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPMWlFIUUN3ME24OE4xOTl5IN88US=> Mnz5V2FPT0WU
KINGS-1 NX7XZYwxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHJOYFKSzVyPUi2MlE3OThizszN MmT2V2FPT0WU
HCC2218 M1KwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXrb5BKSzVyPUi2Mlc6OTNizszN NFXBZXFUSU6JRWK=
GI-ME-N MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknHTWM2OD16Nz63Olk6KM7:TR?= NYnRdYc4W0GQR1XS
AM-38 M2G1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\JV2lEPTB;OEiuN|k2OyEQvF2= NUXkPXRuW0GQR1XS
KNS-42 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLtdpYyUUN3ME24PU4yODF6IN88US=> M1ftdnNCVkeHUh?=
C8166 NIf0ZVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDGeFRKSzVyPUi5MlYyOjVizszN MlLmV2FPT0WU
Ramos-2G6-4C10 NYW3WJpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTh7Lki3NVkh|ryP MlG3V2FPT0WU
CTB-1 NICwWFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS3b2FWUUN3ME25NE43OzV5IN88US=> MnLYV2FPT0WU
HCE-4 NYfUe3YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jWNWlEPTB;OUGuNVM{PiEQvF2= MXPTRW5ITVJ?
NCI-H526 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvXUGFKSzVyPUmyMlQyODNizszN NXu5WmlDW0GQR1XS
ECC4 Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj5dWdTUUN3ME25OE4zPTV3IN88US=> MnLoV2FPT0WU
NCCIT MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PFVmlEPTB;OUWuN|I6OiEQvF2= Mm\OV2FPT0WU
MZ7-mel Mo\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjuWGt4UUN3ME25OU46ODRizszN MXLTRW5ITVJ?
COLO-684 NEKwT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrlXnBKSzVyPUm2MlI{QDVizszN MXHTRW5ITVJ?
SU-DHL-1 NW\QeXY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M36y[GlEPTB;OU[uPVg1OiEQvF2= MUTTRW5ITVJ?
SF126 M3X2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HIbGlEPTB;OUeuOVIyPyEQvF2= Ml70V2FPT0WU
NMC-G1 NFTJUopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rYXGlEPTB;OUiuOFU2PCEQvF2= MVHTRW5ITVJ?
NB14 NFzU[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrhUlFGUUN3ME25PE46OjB6IN88US=> NXTkWlk5W0GQR1XS
VA-ES-BJ NWDNc5g6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLRclhKSzVyPUm5MlQxPTZizszN Mof3V2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-STAT5 / STAT5 ; 

PubMed: 18981115     


For phospho-STAT3 and Phospho-STAT5 detection, cells were then activated for 6 hrs with anti-CD3 and anti-CD28 Ab. Equivalent amounts of protein from cell lysates were separated by SDS-PAGE and western blot analysis was then performed using anti-phospho STAT3, anti-STAT3, anti-phospho STAT5 or anti-STAT5 Abs.

p-ZAP70 / ZAP70 / p-LAT / LAT ; 

PubMed: 18981115     


For the analysis of imatinib interference with early TCR signaling events, cells were activated for 5 min with anti-CD3 and anti-CD28 Abs and blots were probed with anti-phospho ZAP70, anti-ZAP70, anti-phospho LAT or anti-LAT antibodies. Untreated, non-activated cells were used as controls (NA).

p-STAT3 / STAT3 / p-STAT5 / STAT5 ; 

PubMed: 18981115     


For phospho-STAT3 and Phospho-STAT5 detection, cells were then activated for 6 hrs with anti-CD3 and anti-CD28 Ab. Equivalent amounts of protein from cell lysates were separated by SDS-PAGE and western blot analysis was then performed using anti-phospho STAT3, anti-STAT3, anti-phospho STAT5 or anti-STAT5 Abs.

p-ZAP70 / ZAP70 / p-LAT / LAT ; 

PubMed: 18981115     


For the analysis of imatinib interference with early TCR signaling events, cells were activated for 5 min with anti-CD3 and anti-CD28 Abs and blots were probed with anti-phospho ZAP70, anti-ZAP70, anti-phospho LAT or anti-LAT antibodies. Untreated, non-activated cells were used as controls (NA).

18981115
Immunofluorescence
RelB; 

PubMed: 20371728     


Nuclear proteins were extracted from the untreated and treated cells and nuclear levels of RelA and RelB were confirmed by immunocytochemistry 

Cortactin / F-actin ; 

PubMed: 20937825     


NIH3T3-SrcY527F cells were treated with DMSO or with 10 μm STI571 for 16 h, fixed and co-stained for cortactin (red, left panels) and F-actin (green, middle panels). Merged fields (right panels) demonstrate co-localization between cortactin and F-actin at invadopodia.

RelB; 

PubMed: 20371728     


Nuclear proteins were extracted from the untreated and treated cells and nuclear levels of RelA and RelB were confirmed by immunocytochemistry.

Cortactin / F-actin ; 

PubMed: 20937825     


NIH3T3-SrcY527F cells were treated with DMSO or with 10 μm STI571 for 16 h, fixed and co-stained for cortactin (red, left panels) and F-actin (green, middle panels). Merged fields (right panels) demonstrate co-localization between cortactin and F-actin at invadopodia.

20371728 20937825
Growth inhibition assay
Cell viability ; 

PubMed: 28435223     


(C) K562 cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. (D) KBM7R cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. Mean ± SD. n=3. *P<0.05, compared to the control group. #P<0.05, compared to the group of IM alone. Abbreviations: IM, imatinib; SD, standard deviation.

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

Kinase Assay:

[1]

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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]

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  • 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.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
  • Formulation: Imatinib is diluted in water.
  • Dosages: 70 or 100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

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

* 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 493.6
Formula

C29H31N7O

CAS No. 152459-95-5
Storage powder
in solvent
Synonyms CGP057148B, ST-1571

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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    V2

* 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

  • Computed Result

  • 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):
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    C8=C7/X C8: LOG(C8):
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

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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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
NCT04097093 Not yet recruiting Other: No intervention GIST European Organisation for Research and Treatment of Cancer - EORTC December 1 2019 --
NCT03997903 Not yet recruiting Drug: Imatinib Mesylate Sickle Cell Disease Indiana University|Purdue University|Children''s Hospital Medical Center Cincinnati September 2019 Early Phase 1
NCT03891901 Not yet recruiting Drug: Imatinib|Drug: Isoniazid|Drug: Rifabutin Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) September 2019 Phase 2
NCT02644525 Recruiting Drug: Imatinib Mesylate|Drug: Placebo Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) September 16 2019 Phase 2
NCT03578367 Recruiting Drug: Asciminib add-on|Drug: Imatinib|Drug: Nilotinib CML|Chronic Myelogenous Leukemia|Leukemia Myeloid Chronic|Hematologic Diseases Novartis Pharmaceuticals|Novartis November 22 2018 Phase 2
NCT03454503 Not yet recruiting Drug: Imatinib Philadelphia Chromosome-positive Chronic Myeloid Leukemia in Chronic Phase Hikma Pharmaceuticals LLC May 2018 --

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID