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 v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.

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Cited by 33 Publications

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  • Ba/F3-p210T315I cells were treated with indicated concentrations of imatinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

    FASEB J 2011 25, 3661-3673. Imatinib (STI571) purchased from Selleck.

     

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with imatinib. K562 cells (a and c) and MEG-01 cells (b and d) were incubated at 37 ◦C for 15 min with imatinib transport buffer, and then incubated with 0.5 Ci of [3H] thymidine or [3H] cytarabine for an additional 5 min in presence of imatinib. Cells were then washed 3 times, lysed and radioactivity associated to cell pellets was quantified. DMSO, dimethylsulfoxide; DPD, dipyridamole.

    Leukemia Res 2012 36, 1311-1314. Imatinib (STI571) purchased from Selleck.

  • Cell Viability assay results. A2C12, BetaD5, GammaA3, GammaD12, A549, CaCo2, HepG2 cell lines were treated with imatinib mesylate for 24h and 96h.

    Dr. Thomas Kruwel of Fraunhofer. Imatinib (STI571) purchased from Selleck.

    A. Viability curve for the c-Kit mutant MelMS melanoma cell line treated with increasing concentrations of imatinib for 72h (relative to DMSO-treated controls; mean ±sd; n=3) B. MelMS melanoma cells were treated with 50nM imatinib for 24h. The effects on c-Kit, ERK and AKT activation were determined by immunoblotting.

    Dr. Helen Rizos from the university of Sydney. Imatinib (STI571) purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 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 M2PQcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTDUWNrUUN3ME2wMlA4OzB2IN88US=> Mnq0V2FPT0WU
EM-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NICwXlNKSzVyPUCuNFg5QCEQvF2= M{XsZXNCVkeHUh?=
MEG-01 Mo\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\oTWM2OD1yLkC4PVIyKM7:TR?= NHTnOplUSU6JRWK=
BV-173 M33hb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\0UWlEPTB;MD6xPFc1KM7:TR?= MoH3V2FPT0WU
K-562 M{XGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zZWGlEPTB;MD6yNlQ{OiEQvF2= NI\LcXZUSU6JRWK=
CGTH-W-1 NITwelZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfoO2pKSzVyPUCuN|g{PzRizszN NF\5[oVUSU6JRWK=
ST486 M1Ts[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTHSI9jUUN3ME2wMlY5PTRizszN MV7TRW5ITVJ?
NCI-H1436 M{Dhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES5VGRKSzVyPUCuPVc5ODFizszN NGHaRllUSU6JRWK=
NOS-1 M3O5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK3c21mUUN3ME2xMlY2Ozh|IN88US=> M{iyVnNCVkeHUh?=
A498 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfHTWM2OD1{LkW3NlI{KM7:TR?= MkHyV2FPT0WU
BE-13 NEfPfHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO0cphlUUN3ME2yMlYzOTB4IN88US=> NVrqXFZEW0GQR1XS
SUP-T1 NY[yeZhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTNwOEK5NFch|ryP M4PuenNCVkeHUh?=
NCI-H1770 NGnobmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTVwNUeyOlIh|ryP MULTRW5ITVJ?
IMR-5 NUPMd2MzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLUOYtbUUN3ME22MlIzOTR5IN88US=> M{nzWHNCVkeHUh?=
LB2241-RCC M{jjXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXKU4hKSzVyPUiuNFc{QDRizszN MWnTRW5ITVJ?
TGBC24TKB M{TIW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;KeoRlUUN3ME24MlM1ODV{IN88US=> MlG4V2FPT0WU
SCC-15 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\aSZhGUUN3ME2xNE44Pzh6IN88US=> NUn2OXJTW0GQR1XS
BB49-HNC M{jGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTF2LkOzN|Uh|ryP MnXoV2FPT0WU
ES7 NIPhN4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnH[GdKSzVyPUG0Mlc{PzlizszN NGDqZoNUSU6JRWK=
LB2518-MEL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTETWM2OD1zNj62NFk1KM7:TR?= NFvqfFJUSU6JRWK=
NCI-H510A MlfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLZR|RuUUN3ME2xO{4zPDR{IN88US=> MV7TRW5ITVJ?
TE-441-T NXzSTFF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC3TWM2OD1zNz6yPFg3KM7:TR?= M4HUe3NCVkeHUh?=
HH M3vlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLSTWM2OD1zNz6zPVk6KM7:TR?= NHTpSG1USU6JRWK=
LC4-1 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rUSWlEPTB;MUiuNFY2OiEQvF2= MVPTRW5ITVJ?
KARPAS-45 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nCOmlEPTB;MUiuNVg1QCEQvF2= MoXxV2FPT0WU
LB1047-RCC MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfaTWM2OD1zOD60OFUzKM7:TR?= MWTTRW5ITVJ?
NKM-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK3W4lsUUN3ME2xPU4{PTV{IN88US=> NGHCfGxUSU6JRWK=
SCLC-21H MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\rfYNoUUN3ME2yNE4yOjR4IN88US=> M{f5enNCVkeHUh?=
RS4-11 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJyLkOzNFgh|ryP NHfIV5FUSU6JRWK=
ALL-PO NVrVdJFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHweVlNUUN3ME2yNE45OTR7IN88US=> NI\2UGpUSU6JRWK=
GDM-1 NXPubFBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJ{LkW5OFUh|ryP MXHTRW5ITVJ?
DMS-79 NHK1V4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJ2LkS5N|Qh|ryP NH:0Z|hUSU6JRWK=
MPP-89 NWS5WFhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYntRVFKUUN3ME2yOU43QDd2IN88US=> M1X2fHNCVkeHUh?=
NB10 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[5S296UUN3ME2yOk41Pjl7IN88US=> M{jXfnNCVkeHUh?=
LS-513 NXTaNot3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfHTWM2OD1{Nj64PFQ4KM7:TR?= MUHTRW5ITVJ?
L-540 NHH2VYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETWPFBKSzVyPUK2MlkyPDNizszN M1XkTnNCVkeHUh?=
ES1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJ5LkWyNUDPxE1? NYG3WYJEW0GQR1XS
NTERA-S-cl-D1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjUTWM2OD1|MD61NFk{KM7:TR?= MYPTRW5ITVJ?
EW-1 NH3FZZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrIWHVKSzVyPUOyMlk1PTRizszN MXfTRW5ITVJ?
Calu-6 NUXZR5l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj2TWM2OD1|Mz6xPFU2KM7:TR?= MUXTRW5ITVJ?
CTV-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\xZmZKSzVyPUOzMlk4QDlizszN MoPhV2FPT0WU
YT M3yxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fRPGlEPTB;M{iuOVIxQSEQvF2= M1X2RnNCVkeHUh?=
TE-6 NGXJ[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPBdo1KSzVyPUSxMlI4QThizszN NEfoenRUSU6JRWK=
HT-144 NGnUWIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HDOGlEPTB;NEGuOVQ5PiEQvF2= M4X4NXNCVkeHUh?=
EW-13 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTR{LkK3PVEh|ryP MXHTRW5ITVJ?
KALS-1 M4Dwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LRZ2lEPTB;NEOuNVMzQSEQvF2= NEG2OGNUSU6JRWK=
MOLT-16 NVm2bWE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkCzTWM2OD12NT6wO|UzKM7:TR?= MXTTRW5ITVJ?
D-336MG M{LCUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR3Lkm1PVkh|ryP M1faSnNCVkeHUh?=
TE-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHhTWM2OD12Nj62OVMh|ryP NGLRNppUSU6JRWK=
EB2 M{Dicmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTR4Lk[5PUDPxE1? NX;HbJNbW0GQR1XS
SK-N-DZ M4jLW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR6LkC5OlEh|ryP MWLTRW5ITVJ?
SW684 NUCzUnM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR6LkK2PVUh|ryP MYHTRW5ITVJ?
EW-18 NWfXNWFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:5NnFKSzVyPUS4MlQ{QTVizszN M{f5W3NCVkeHUh?=
RL95-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEH3OWlKSzVyPUWwMlA4OSEQvF2= M4DxZ3NCVkeHUh?=
CHP-126 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTVyLki5NFUh|ryP NUHrfJlnW0GQR1XS
NCI-H1395 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nCeWlEPTB;NUGuO|g{PSEQvF2= NV\aOGs2W0GQR1XS
TE-15 M4XrRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjFTWM2OD13Mj6yOVU3KM7:TR?= MXfTRW5ITVJ?
ES4 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfJd|FKSzVyPUWyMlk4PzVizszN M4robHNCVkeHUh?=
TE-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXDTWM2OD13Mz65OFU2KM7:TR?= NFLpfWxUSU6JRWK=
SIMA MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fDTWlEPTB;NUeuN|MyOSEQvF2= NXn5W|hLW0GQR1XS
LB647-SCLC NGn1UFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi4[m1[UUN3ME22OE4yOTh6IN88US=> NWP5XlVxW0GQR1XS
KY821 NGTXNIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPINpdCUUN3ME22OE4zPTV{IN88US=> M{PkS3NCVkeHUh?=
LC-2-ad MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nUTWlEPTB;NkWuO|YxOSEQvF2= MUPTRW5ITVJ?
KP-N-RT-BM-1 NXvhcIJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTZ4Lk[zOlYh|ryP NHjDb|dUSU6JRWK=
SW872 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjOSFdGUUN3ME22O{41Ozh{IN88US=> M{OyRnNCVkeHUh?=
ES5 NYHqOnBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HXdWlEPTB;NkeuOlk3QCEQvF2= MYjTRW5ITVJ?
SK-NEP-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DwdmlEPTB;NkiuN|gxOyEQvF2= MV3TRW5ITVJ?
RPMI-6666 M2raNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTdzLkCzNkDPxE1? NHrDTYNUSU6JRWK=
UACC-812 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLHfWlwUUN3ME23NU4yPjB7IN88US=> MVfTRW5ITVJ?
COLO-829 NXXjb|YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTd{Lk[5PFch|ryP Mo\kV2FPT0WU
KP-N-YS M2HqS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTd{LkexN|kh|ryP NE\aeoVUSU6JRWK=
GI-1 NF[0b|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfUTWM2OD15Mz6yPFY5KM7:TR?= NFT4VIFUSU6JRWK=
ETK-1 NHnCXJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLNU2VWUUN3ME23N{41QTN{IN88US=> M1fPfnNCVkeHUh?=
LXF-289 M3uzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTd|LkeyPUDPxE1? MVLTRW5ITVJ?
CAS-1 Mk\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jxWGlEPTB;N{OuPFg2PyEQvF2= NHfrUYdUSU6JRWK=
EW-22 M1\FZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq4VJhKSzVyPUe0MlcyOTVizszN Mke3V2FPT0WU
NCI-H2196 M4fQW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTd3Lk[zO|kh|ryP NFXPT5RUSU6JRWK=
EoL-1-cell M1u1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTtN3dVUUN3ME24NU43QTZ|IN88US=> M4XDWHNCVkeHUh?=
D-247MG Mk\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3MVFFKSzVyPUiyMlAzPDhizszN NV7UU446W0GQR1XS
Becker NVvrVIVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDyTWM2OD16Mj6zOFgyKM7:TR?= NF7wSoJUSU6JRWK=
IST-MEL1 MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7ZNIJKSzVyPUiyMlM1QDJizszN NHe5XllUSU6JRWK=
MDA-MB-134-VI M1;WeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHiTWM2OD16Mj61PVk3KM7:TR?= NHrLZmZUSU6JRWK=
NCI-H1092 MorUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHp[VBKSzVyPUi0MlAyQTdizszN NIrHSolUSU6JRWK=
KINGS-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjTSWFKSzVyPUi2MlE3OThizszN MofPV2FPT0WU
HCC2218 M1PJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7QUW52UUN3ME24Ok44QTF|IN88US=> MkDsV2FPT0WU
GI-ME-N M{izeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTh5Lke2PVkh|ryP NEnMXWpUSU6JRWK=
AM-38 NWS3cZRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTh6LkO5OVMh|ryP MX\TRW5ITVJ?
KNS-42 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPVTWM2OD16OT6xNFE5KM7:TR?= NHHTOYFUSU6JRWK=
C8166 NHfZPZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fOUGlEPTB;OEmuOlEzPSEQvF2= NYLDcFF[W0GQR1XS
Ramos-2G6-4C10 MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGi4PZhKSzVyPUi5Mlg4OTlizszN MUfTRW5ITVJ?
CTB-1 MnrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPFfW1KSzVyPUmwMlY{PTdizszN Mn:5V2FPT0WU
HCE-4 MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTlzLkGzN|Yh|ryP NFLkNpdUSU6JRWK=
NCI-H526 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnrTWM2OD17Mj60NVA{KM7:TR?= MkLZV2FPT0WU
ECC4 M2L0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHDPWtKUUN3ME25OE4zPTV3IN88US=> NVuxflVJW0GQR1XS
NCCIT NF64eGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnI[JZLUUN3ME25OU4{Ojl{IN88US=> M4DVUHNCVkeHUh?=
MZ7-mel M3LCOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDXUVRKSzVyPUm1MlkxPCEQvF2= MXvTRW5ITVJ?
COLO-684 NUK3VmZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTl4LkKzPFUh|ryP M3G2XnNCVkeHUh?=
SU-DHL-1 NH7BbolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jxNmlEPTB;OU[uPVg1OiEQvF2= MknYV2FPT0WU
SF126 NX7VXlJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\iOm5KSzVyPUm3MlUzOTdizszN NYDNNIJWW0GQR1XS
NMC-G1 Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTUR4JnUUN3ME25PE41PTV2IN88US=> M2[4TXNCVkeHUh?=
NB14 MnvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvsS2MyUUN3ME25PE46OjB6IN88US=> NFnOe49USU6JRWK=
VA-ES-BJ MnX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[0UYhKSzVyPUm5MlQxPTZizszN MY\TRW5ITVJ?

... Click to View More Cell Line Experimental Data

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
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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
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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
+ Expand
  • 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 4 mg/mL (8.1 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* 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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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
    V1
    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 Conditions Sponsor/Collaborators Start Date Phases
NCT02709083 Not yet recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University December 2016 Phase 2
NCT02812693 Not yet recruiting Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma Joanne Jeter|National Cancer Institute (NCI)|Merck Ltd.|Ohio State University Comprehensive Cancer Center September 2016 Phase 1|Phase 2
NCT02538926 Not yet recruiting B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T Lymphoblastic Leukemia/Lymphoma|Refractory B Lymphoblastic Lymphoma|Refractory T Lymphoblastic Lymphoma|T Acute Lymphoblastic Leukemia|T Lymphoblastic Lymphoma University of Washington|National Cancer Institute (NCI) August 2016 Phase 2
NCT02685046 Recruiting Colonic Neoplasms UMC Utrecht|Meander Medical Center|Erasmus Medical Center|Hubrecht Institute April 2016 Phase 2
NCT02611492 Recruiting Philadelphia Chromosome Positive Adult Acute Lymphoblastic Leukemia Assistance Publique - Hôpitaux de Paris April 2016 Phase 3
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto March 2016 Phase 4

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:

    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