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 72 Publications

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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 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrPUpdKSzVyPUCuNFc{ODRizszN NHHuXnJUSU6JRWK=
EM-2 M3XDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13pc2lEPTB;MD6wPFg5KM7:TR?= NITtbVNUSU6JRWK=
MEG-01 NGrQTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwMEi5NlEh|ryP Mlr0V2FPT0WU
BV-173 NFzRUVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmiwTWM2OD1yLkG4O|Qh|ryP NX:z[ZhXW0GQR1XS
K-562 M1;vW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXz4fWxDUUN3ME2wMlIzPDN{IN88US=> MkHjV2FPT0WU
CGTH-W-1 NUW5SVBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX2xdZllUUN3ME2wMlM5Ozd2IN88US=> MUXTRW5ITVJ?
ST486 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr4blhDUUN3ME2wMlY5PTRizszN M{ezPHNCVkeHUh?=
NCI-H1436 NEP6cVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fRNGlEPTB;MD65O|gxOSEQvF2= M{TWPXNCVkeHUh?=
NOS-1 NWLOWWh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGW3N|BKSzVyPUGuOlU{QDNizszN NXqzS25WW0GQR1XS
A498 NYfxPY97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnUdnJVUUN3ME2yMlU4OjJ|IN88US=> NFnNWYpUSU6JRWK=
BE-13 NFrW[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrWSWRQUUN3ME2yMlYzOTB4IN88US=> NEnOOlJUSU6JRWK=
SUP-T1 NHXUN2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnDXllKSzVyPUOuPFI6ODdizszN NIjWSIZUSU6JRWK=
NCI-H1770 NVXpdFJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVG1U|huUUN3ME21MlU4OjZ{IN88US=> NF\SXYJUSU6JRWK=
IMR-5 MnvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTuTWM2OD14LkKyNVQ4KM7:TR?= MWTTRW5ITVJ?
LB2241-RCC M4e1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7ZTWM2OD16LkC3N|g1KM7:TR?= MnK1V2FPT0WU
TGBC24TKB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRThwM{SwOVIh|ryP NIXwO4ZUSU6JRWK=
SCC-15 Ml\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m4UGlEPTB;MUCuO|c5QCEQvF2= M{XD[HNCVkeHUh?=
BB49-HNC NIj1NHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37wfWlEPTB;MUSuN|M{PSEQvF2= NH3vVYNUSU6JRWK=
ES7 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFq3OIpKSzVyPUG0Mlc{PzlizszN NWPRdZd6W0GQR1XS
LB2518-MEL M2qzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTF4Lk[wPVQh|ryP MofwV2FPT0WU
NCI-H510A NFXnO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXftV3RtUUN3ME2xO{4zPDR{IN88US=> MUXTRW5ITVJ?
TE-441-T NUH5S2g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rTbWlEPTB;MUeuNlg5PiEQvF2= MkfyV2FPT0WU
HH NWT3NVJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X1PWlEPTB;MUeuN|k6QSEQvF2= MlHFV2FPT0WU
LC4-1 NI\VRnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrJ[GlKSzVyPUG4MlA3PTJizszN M{HsfnNCVkeHUh?=
KARPAS-45 M162Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L2dmlEPTB;MUiuNVg1QCEQvF2= MXrTRW5ITVJ?
LB1047-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF6LkS0OVIh|ryP NGjwVpRUSU6JRWK=
NKM-1 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nDPGlEPTB;MUmuN|U2OiEQvF2= M1TVZ3NCVkeHUh?=
SCLC-21H MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXhT5BbUUN3ME2yNE4yOjR4IN88US=> M{\wW3NCVkeHUh?=
RS4-11 NUXkbXRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjZTWM2OD1{MD6zN|A5KM7:TR?= NIrSXo9USU6JRWK=
ALL-PO NIHST2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLkWJpOUUN3ME2yNE45OTR7IN88US=> NVTybI1VW0GQR1XS
GDM-1 M2TibGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PEWGlEPTB;MkKuOVk1PSEQvF2= Mlj6V2FPT0WU
DMS-79 NEizVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjIOm4yUUN3ME2yOE41QTN2IN88US=> MnPPV2FPT0WU
MPP-89 MlnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTJ3Lk[4O|Qh|ryP M1LLSnNCVkeHUh?=
NB10 M2CzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHFTWM2OD1{Nj60Olk6KM7:TR?= MlL2V2FPT0WU
LS-513 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HYbmlEPTB;Mk[uPFg1PyEQvF2= MW\TRW5ITVJ?
L-540 NILCSY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJ4LkmxOFMh|ryP M{fnbXNCVkeHUh?=
ES1 M1zLcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\aRVROUUN3ME2yO{42OjFizszN NV\pRnZjW0GQR1XS
NTERA-S-cl-D1 NI\GSGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTNyLkWwPVMh|ryP NH3LWIdUSU6JRWK=
EW-1 NXvaPJVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTN{Lkm0OVQh|ryP MkXMV2FPT0WU
Calu-6 NHXGV45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HaPWlEPTB;M{OuNVg2PSEQvF2= M3nEWXNCVkeHUh?=
CTV-1 M4jHcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;QUIhRUUN3ME2zN{46Pzh7IN88US=> MkG3V2FPT0WU
YT Mnr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37pfmlEPTB;M{iuOVIxQSEQvF2= NF\SXoRUSU6JRWK=
TE-6 NViyVWhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\UTFhnUUN3ME20NU4zPzl6IN88US=> NVHYfYppW0GQR1XS
HT-144 NUDqOlVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvKTWM2OD12MT61OFg3KM7:TR?= MkHMV2FPT0WU
EW-13 NV\4dHpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XVOGlEPTB;NEKuNlc6OSEQvF2= MoXVV2FPT0WU
KALS-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7OTWM2OD12Mz6xN|I6KM7:TR?= M4ixU3NCVkeHUh?=
MOLT-16 NWjhU|hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LjT2lEPTB;NEWuNFc2OiEQvF2= M3XUW3NCVkeHUh?=
D-336MG Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjrVpJKSzVyPUS1Mlk2QTlizszN NGG5WolUSU6JRWK=
TE-11 M3;SbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTSTnhKSzVyPUS2MlY2OyEQvF2= NWDmXXpoW0GQR1XS
EB2 M2LSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVeyXWdlUUN3ME20Ok43QTlizszN MnfBV2FPT0WU
SK-N-DZ MoLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD6TWM2OD12OD6wPVYyKM7:TR?= NGnh[3BUSU6JRWK=
SW684 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PjT2lEPTB;NEiuNlY6PSEQvF2= MUHTRW5ITVJ?
EW-18 NEfMOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPHNFhKSzVyPUS4MlQ{QTVizszN NYfVUHJMW0GQR1XS
RL95-2 NFnJcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzZTWM2OD13MD6wO|Eh|ryP NELtXHZUSU6JRWK=
CHP-126 M4jlR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M321S2lEPTB;NUCuPFkxPSEQvF2= MnnEV2FPT0WU
NCI-H1395 NITSeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPZemRUUUN3ME21NU44QDN3IN88US=> MWXTRW5ITVJ?
TE-15 NEfFSJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzudIJKSzVyPUWyMlI2PTZizszN M3vhSXNCVkeHUh?=
ES4 M3HIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTsTWM2OD13Mj65O|c2KM7:TR?= M2TKS3NCVkeHUh?=
TE-1 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjPTWM2OD13Mz65OFU2KM7:TR?= MVjTRW5ITVJ?
SIMA M2n5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrLUotqUUN3ME21O{4{OzFzIN88US=> MXvTRW5ITVJ?
LB647-SCLC MlOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LKWmlEPTB;NkSuNVE5QCEQvF2= Moe0V2FPT0WU
KY821 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;EeXROUUN3ME22OE4zPTV{IN88US=> NVu4OVhSW0GQR1XS
LC-2-ad MnLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTZ3Lke2NFEh|ryP NH7sZpJUSU6JRWK=
KP-N-RT-BM-1 NXHMT3VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTZ4Lk[zOlYh|ryP NITCe2hUSU6JRWK=
SW872 MnOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLEUGFKSzVyPU[3MlQ{QDJizszN MWHTRW5ITVJ?
ES5 M{H3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTZ5Lk[5Olgh|ryP MY\TRW5ITVJ?
SK-NEP-1 M3vydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TmdGlEPTB;NkiuN|gxOyEQvF2= NEHMOWFUSU6JRWK=
RPMI-6666 NYnEenNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXmTWM2OD15MT6wN|Ih|ryP NX7OfppNW0GQR1XS
UACC-812 M1GzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfCcJV1UUN3ME23NU4yPjB7IN88US=> MlHvV2FPT0WU
COLO-829 M4SzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHofYd2UUN3ME23Nk43QTh5IN88US=> MYDTRW5ITVJ?
KP-N-YS NYPVTVBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzkTWM2OD15Mj63NVM6KM7:TR?= NYm5fYRYW0GQR1XS
GI-1 M1nveGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUOzbWIyUUN3ME23N{4zQDZ6IN88US=> M{PNeXNCVkeHUh?=
ETK-1 MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDkNIJKSzVyPUezMlQ6OzJizszN NF\6c5ZUSU6JRWK=
LXF-289 NGLkUnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPPUXpKSzVyPUezMlczQSEQvF2= MXHTRW5ITVJ?
CAS-1 NGnMVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrjTmJKSzVyPUezMlg5PTdizszN Mn;0V2FPT0WU
EW-22 M4rCeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXP1c|c2UUN3ME23OE44OTF3IN88US=> NXnEdVQzW0GQR1XS
NCI-H2196 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPaTWM2OD15NT62N|c6KM7:TR?= MoDBV2FPT0WU
EoL-1-cell MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XUSWlEPTB;OEGuOlk3OyEQvF2= M3GxUXNCVkeHUh?=
D-247MG M33nSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDwUmo5UUN3ME24Nk4xOjR6IN88US=> NX:zeXQyW0GQR1XS
Becker NV\ReJZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;ZTWM2OD16Mj6zOFgyKM7:TR?= M{i3enNCVkeHUh?=
IST-MEL1 MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTh{LkO0PFIh|ryP MoW1V2FPT0WU
MDA-MB-134-VI M{PITGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7M[nNCUUN3ME24Nk42QTl4IN88US=> M{nMOnNCVkeHUh?=
NCI-H1092 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTh2LkCxPVch|ryP MnjrV2FPT0WU
KINGS-1 NXv0N3NCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q4S2lEPTB;OE[uNVYyQCEQvF2= MXvTRW5ITVJ?
HCC2218 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPo[WM3UUN3ME24Ok44QTF|IN88US=> M3;vN3NCVkeHUh?=
GI-ME-N Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDuZlBKSzVyPUi3Mlc3QTlizszN M{\rZ3NCVkeHUh?=
AM-38 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIft[nRKSzVyPUi4MlM6PTNizszN MVrTRW5ITVJ?
KNS-42 MnfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP0TWM2OD16OT6xNFE5KM7:TR?= MUDTRW5ITVJ?
C8166 Mn73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH3SVBKSzVyPUi5MlYyOjVizszN MVvTRW5ITVJ?
Ramos-2G6-4C10 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;xUHNKSzVyPUi5Mlg4OTlizszN NUDWV2VGW0GQR1XS
CTB-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M164Z2lEPTB;OUCuOlM2PyEQvF2= MnTxV2FPT0WU
HCE-4 MoL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvWN29lUUN3ME25NU4yOzN4IN88US=> NYT0Z5hpW0GQR1XS
NCI-H526 NGHQR3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTl{LkSxNFMh|ryP Mlf4V2FPT0WU
ECC4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PVe2lEPTB;OUSuNlU2PSEQvF2= MVTTRW5ITVJ?
NCCIT M3rQfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjpdpR{UUN3ME25OU4{Ojl{IN88US=> MW\TRW5ITVJ?
MZ7-mel M2jOVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUmxRY9iUUN3ME25OU46ODRizszN NFzMXldUSU6JRWK=
COLO-684 NFfTWZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTl4LkKzPFUh|ryP NWXN[XJbW0GQR1XS
SU-DHL-1 NHPHN4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rmdmlEPTB;OU[uPVg1OiEQvF2= NHrlNY9USU6JRWK=
SF126 NUG0elh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjxdnRKSzVyPUm3MlUzOTdizszN Mn:xV2FPT0WU
NMC-G1 M3;iVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fLU2lEPTB;OUiuOFU2PCEQvF2= MnK1V2FPT0WU
NB14 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j2WGlEPTB;OUiuPVIxQCEQvF2= M2XMVHNCVkeHUh?=
VA-ES-BJ Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTl7LkSwOVYh|ryP NFXHeXhUSU6JRWK=

... 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:

[1]

+ Expand

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]

+ Expand
  • 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]

+ 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 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

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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 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