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 105 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 NHHjVWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXyTWM2OD1yLkC3N|A1KM7:TR?= NYHQVYNtW0GQR1XS
EM-2 NIfQVXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy0WFJKSzVyPUCuNFg5QCEQvF2= Mo\2V2FPT0WU
MEG-01 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXveFdKSzVyPUCuNFg6OjFizszN M2\yOXNCVkeHUh?=
BV-173 NGnlSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2W4PWlEPTB;MD6xPFc1KM7:TR?= NYTONm1yW0GQR1XS
K-562 M4DzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLuTWM2OD1yLkKyOFMzKM7:TR?= MVXTRW5ITVJ?
CGTH-W-1 MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO0TG1KSzVyPUCuN|g{PzRizszN NFThVHpUSU6JRWK=
ST486 NX36THVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwNki1OEDPxE1? NE\CemFUSU6JRWK=
NCI-H1436 M4HsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j5ZWlEPTB;MD65O|gxOSEQvF2= M{PVPHNCVkeHUh?=
NOS-1 Ml6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnD[XBKSzVyPUGuOlU{QDNizszN NWnnfYtTW0GQR1XS
A498 M33vT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M32yXmlEPTB;Mj61O|IzOyEQvF2= NXXqdHI6W0GQR1XS
BE-13 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjCR|FqUUN3ME2yMlYzOTB4IN88US=> MlHQV2FPT0WU
SUP-T1 NFKzR49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTNwOEK5NFch|ryP MXXTRW5ITVJ?
NCI-H1770 MoPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fiXGlEPTB;NT61O|I3OiEQvF2= M{\oUXNCVkeHUh?=
IMR-5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTBTWM2OD14LkKyNVQ4KM7:TR?= NV;uW3RRW0GQR1XS
LB2241-RCC MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPPTWM2OD16LkC3N|g1KM7:TR?= NX32PIs4W0GQR1XS
TGBC24TKB NILTWItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\6TWM2OD16LkO0NFUzKM7:TR?= M2TuTnNCVkeHUh?=
SCC-15 NIO3XlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTFyLke3PFgh|ryP MYDTRW5ITVJ?
BB49-HNC MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LaSWlEPTB;MUSuN|M{PSEQvF2= NFy3cmVUSU6JRWK=
ES7 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF2LkezO|kh|ryP NV31TYs4W0GQR1XS
LB2518-MEL Mn63S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;3ZopLUUN3ME2xOk43ODl2IN88US=> M1HoW3NCVkeHUh?=
NCI-H510A NFTJd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvlUnpKSzVyPUG3MlI1PDJizszN M2qzfnNCVkeHUh?=
TE-441-T NFfQdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnCTWM2OD1zNz6yPFg3KM7:TR?= MV\TRW5ITVJ?
HH NF;UR5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi1TWtKSzVyPUG3MlM6QTlizszN MWDTRW5ITVJ?
LC4-1 NEPkVHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TqVGlEPTB;MUiuNFY2OiEQvF2= NIjHSYpUSU6JRWK=
KARPAS-45 NGfsUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnn5TWM2OD1zOD6xPFQ5KM7:TR?= MnjxV2FPT0WU
LB1047-RCC Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vUcGlEPTB;MUiuOFQ2OiEQvF2= MVrTRW5ITVJ?
NKM-1 NX3TdFVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELn[4RKSzVyPUG5MlM2PTJizszN NHzjfXFUSU6JRWK=
SCLC-21H MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;C[nR2UUN3ME2yNE4yOjR4IN88US=> MVnTRW5ITVJ?
RS4-11 NWPPUGtST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLITWM2OD1{MD6zN|A5KM7:TR?= MkC1V2FPT0WU
ALL-PO MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJyLkixOFkh|ryP MlHCV2FPT0WU
GDM-1 Ml\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPKTWM2OD1{Mj61PVQ2KM7:TR?= NFvk[|NUSU6JRWK=
DMS-79 M1LqOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vjbWlEPTB;MkSuOFk{PCEQvF2= MUXTRW5ITVJ?
MPP-89 NFPTSnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPzSmZQUUN3ME2yOU43QDd2IN88US=> Mo\rV2FPT0WU
NB10 NY\VWJBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLOe49KSzVyPUK2MlQ3QTlizszN MVnTRW5ITVJ?
LS-513 NGnrRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJ4Lki4OFch|ryP MUXTRW5ITVJ?
L-540 NEL2XXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrUTWM2OD1{Nj65NVQ{KM7:TR?= MV;TRW5ITVJ?
ES1 Mn3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ5LkWyNUDPxE1? NYTWSmp7W0GQR1XS
NTERA-S-cl-D1 NUiwXZpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H4[mlEPTB;M{CuOVA6OyEQvF2= NUnp[oRHW0GQR1XS
EW-1 NYLWVG5yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN{Lkm0OVQh|ryP M{\IS3NCVkeHUh?=
Calu-6 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTN|LkG4OVUh|ryP NG\HVWpUSU6JRWK=
CTV-1 NXPxToNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN|Lkm3PFkh|ryP NYTLdIptW0GQR1XS
YT M2nZfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrJTWM2OD1|OD61NlA6KM7:TR?= NX;m[5g6W0GQR1XS
TE-6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DWRmlEPTB;NEGuNlc6QCEQvF2= MnjZV2FPT0WU
HT-144 M1\Db2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLqTWM2OD12MT61OFg3KM7:TR?= MWrTRW5ITVJ?
EW-13 NFGyVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTR{LkK3PVEh|ryP NFfsdnFUSU6JRWK=
KALS-1 NXPncot3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTMTWM2OD12Mz6xN|I6KM7:TR?= NGnJcXVUSU6JRWK=
MOLT-16 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTR3LkC3OVIh|ryP NYPsR2c2W0GQR1XS
D-336MG NVzCe|k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTGcVhKSzVyPUS1Mlk2QTlizszN MVjTRW5ITVJ?
TE-11 M1e5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;6ZWlEPTB;NE[uOlU{KM7:TR?= MXTTRW5ITVJ?
EB2 MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXVTWM2OD12Nj62PVkh|ryP MXTTRW5ITVJ?
SK-N-DZ NXzKTZprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\PfXROUUN3ME20PE4xQTZzIN88US=> MnzHV2FPT0WU
SW684 M{TFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nyWWlEPTB;NEiuNlY6PSEQvF2= MmTqV2FPT0WU
EW-18 NIH3R4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYG0V5V1UUN3ME20PE41Ozl3IN88US=> NYjzT3RrW0GQR1XS
RL95-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTVyLkC3NUDPxE1? NYf1bWl3W0GQR1XS
CHP-126 M{fWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTVyLki5NFUh|ryP NXvZWXFFW0GQR1XS
NCI-H1395 NH3B[m9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPZS5lZUUN3ME21NU44QDN3IN88US=> MWjTRW5ITVJ?
TE-15 NEno[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;MTWM2OD13Mj6yOVU3KM7:TR?= MlLtV2FPT0WU
ES4 NWe0eY5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nTTmlEPTB;NUKuPVc4PSEQvF2= MnLmV2FPT0WU
TE-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[ycmlEPTB;NUOuPVQ2PSEQvF2= NF;wbXdUSU6JRWK=
SIMA NVrsV5lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XCbmlEPTB;NUeuN|MyOSEQvF2= NFHHRmVUSU6JRWK=
LB647-SCLC MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjKb2w2UUN3ME22OE4yOTh6IN88US=> M4H5enNCVkeHUh?=
KY821 NFLBdXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W2SWlEPTB;NkSuNlU2OiEQvF2= MlLJV2FPT0WU
LC-2-ad NFniTJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPBb3NKSzVyPU[1Mlc3ODFizszN NVfTTJBFW0GQR1XS
KP-N-RT-BM-1 M2q5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHtRXVKSzVyPU[2MlY{PjZizszN NI[5T4JUSU6JRWK=
SW872 NYry[IdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;Hc2lEPTB;NkeuOFM5OiEQvF2= M2jqcHNCVkeHUh?=
ES5 NUH3RnVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTZ5Lk[5Olgh|ryP M2\4NHNCVkeHUh?=
SK-NEP-1 NF\Ud5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTZ6LkO4NFMh|ryP MXnTRW5ITVJ?
RPMI-6666 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljSTWM2OD15MT6wN|Ih|ryP MWfTRW5ITVJ?
UACC-812 Mnf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPZTWM2OD15MT6xOlA6KM7:TR?= NEjBc4dUSU6JRWK=
COLO-829 NXLLT4JbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTTTWM2OD15Mj62PVg4KM7:TR?= MXLTRW5ITVJ?
KP-N-YS MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDBTWM2OD15Mj63NVM6KM7:TR?= MVLTRW5ITVJ?
GI-1 M1:5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7ZTWM2OD15Mz6yPFY5KM7:TR?= NUi3c2JGW0GQR1XS
ETK-1 NW\vWHBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHvWVhKSzVyPUezMlQ6OzJizszN M2XNRnNCVkeHUh?=
LXF-289 NWTRbFJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LtbGlEPTB;N{OuO|I6KM7:TR?= M4DEOXNCVkeHUh?=
CAS-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[2cGlEPTB;N{OuPFg2PyEQvF2= M{T3Z3NCVkeHUh?=
EW-22 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jOc2lEPTB;N{SuO|EyPSEQvF2= NGi0PYpUSU6JRWK=
NCI-H2196 MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPWTWM2OD15NT62N|c6KM7:TR?= M2\KN3NCVkeHUh?=
EoL-1-cell NUO3XXIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvMfVVkUUN3ME24NU43QTZ|IN88US=> NFj3N5dUSU6JRWK=
D-247MG MkS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G2OGlEPTB;OEKuNFI1QCEQvF2= M1XmTHNCVkeHUh?=
Becker MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzGTWM2OD16Mj6zOFgyKM7:TR?= MYjTRW5ITVJ?
IST-MEL1 MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnpVm5KSzVyPUiyMlM1QDJizszN MXPTRW5ITVJ?
MDA-MB-134-VI M1zlVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi1VWxKSzVyPUiyMlU6QTZizszN MkDyV2FPT0WU
NCI-H1092 NGPK[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPIXFBoUUN3ME24OE4xOTl5IN88US=> MYjTRW5ITVJ?
KINGS-1 NU[3SYt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PnXGlEPTB;OE[uNVYyQCEQvF2= NGO4ZVRUSU6JRWK=
HCC2218 M4PoOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjZTWM2OD16Nj63PVE{KM7:TR?= NV\lc495W0GQR1XS
GI-ME-N MkLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHiSYNOUUN3ME24O{44Pjl7IN88US=> NGK0ZYFUSU6JRWK=
AM-38 M1;jfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rLd2lEPTB;OEiuN|k2OyEQvF2= M4i1Z3NCVkeHUh?=
KNS-42 NUm0e3I4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTh7LkGwNVgh|ryP M3LyOXNCVkeHUh?=
C8166 NWXGWXp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\3PFlIUUN3ME24PU43OTJ3IN88US=> NIHWVGNUSU6JRWK=
Ramos-2G6-4C10 NF2wZ49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rhXWlEPTB;OEmuPFcyQSEQvF2= Mo\ZV2FPT0WU
CTB-1 NYG2W|h3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\rS2hKSzVyPUmwMlY{PTdizszN NV;OVZJEW0GQR1XS
HCE-4 M3;xPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTlzLkGzN|Yh|ryP MYfTRW5ITVJ?
NCI-H526 M{f3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPheZZKSzVyPUmyMlQyODNizszN NFPhelNUSU6JRWK=
ECC4 Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7UR|hKSzVyPUm0MlI2PTVizszN MXTTRW5ITVJ?
NCCIT MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[zTWM2OD17NT6zNlkzKM7:TR?= NEDadXJUSU6JRWK=
MZ7-mel NYLub3RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;F[XJZUUN3ME25OU46ODRizszN NX;OV4VqW0GQR1XS
COLO-684 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P6RmlEPTB;OU[uNlM5PSEQvF2= NETOO5BUSU6JRWK=
SU-DHL-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DtWWlEPTB;OU[uPVg1OiEQvF2= NX7ldpB7W0GQR1XS
SF126 NIjVbJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlroTWM2OD17Nz61NlE4KM7:TR?= MX7TRW5ITVJ?
NMC-G1 NWfRT3JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTl6LkS1OVQh|ryP NEC4[IVUSU6JRWK=
NB14 M4LrZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37hW2lEPTB;OUiuPVIxQCEQvF2= NGPqNIJUSU6JRWK=
VA-ES-BJ NHT4ZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPSWXQ{UUN3ME25PU41ODV4IN88US=> NFztNmlUSU6JRWK=

... 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 )

  • C1
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    C2
    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):
    C7=C6/X C7: LOG(C7):
    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

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
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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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