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 37 Publications

6 Customer Reviews

  • 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.

    Targeting KITLG through c-KIT inhibition using Imatinib; one representative experiment is shown (n = 4).

    Oncotarget, 2016, 7(34):54583-54595. 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.

    ZFX regulates imatinib sensitivity and PI3K/Akt signaling pathway in CML cells. Viability of cells transfected with si-ZFX at the indicated doses of imatinib for 24 h (a). Colonies of leukemia cells and imatinib-resistant cells transfected with si-ZFX following treatment with imatinib for 10 days (b). Western blot analysis of Akt, p-Akt, CyclinD1, CyclinE1, Bcl-2, and Caspase-3 in K562 and K562/G01 cells transfected with si-ZFX for 2 days (c). The relative densities of proteins were quantified and normalized to b-Actin (d). Values represented the mean ± SD data from experiments in triplicate. *P\0.05 and **P\0.01

    Cell Biochem Biophys, 2016, 74(2):277-83. 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

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 NUL5[np{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwMEezNFQh|ryP NUn3RWt3W0GQR1XS
EM-2 M4[4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXCdVJDUUN3ME2wMlA5QDhizszN MkjYV2FPT0WU
MEG-01 MoL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMEi5NlEh|ryP MnS5V2FPT0WU
BV-173 NYHpVVhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml35TWM2OD1yLkG4O|Qh|ryP NHHvOo9USU6JRWK=
K-562 NFrqd|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7pd|A6UUN3ME2wMlIzPDN{IN88US=> M{LTO3NCVkeHUh?=
CGTH-W-1 NEewPJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PLPGlEPTB;MD6zPFM4PCEQvF2= M1;uVnNCVkeHUh?=
ST486 MnjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwNki1OEDPxE1? M4fVRXNCVkeHUh?=
NCI-H1436 MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrpV5BKSzVyPUCuPVc5ODFizszN NGXyeoRUSU6JRWK=
NOS-1 M2H0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnSXlJKSzVyPUGuOlU{QDNizszN MU\TRW5ITVJ?
A498 M2nH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTZNndKSzVyPUKuOVczOjNizszN M1LKeXNCVkeHUh?=
BE-13 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJwNkKxNFYh|ryP M4W3bnNCVkeHUh?=
SUP-T1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13VWWlEPTB;Mz64NlkxPyEQvF2= M2[3NXNCVkeHUh?=
NCI-H1770 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTVwNUeyOlIh|ryP MlzPV2FPT0WU
IMR-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTZwMkKxOFch|ryP MkDpV2FPT0WU
LB2241-RCC NYfaXZZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH1ZZVKUUN3ME24MlA4Ozh2IN88US=> MnLqV2FPT0WU
TGBC24TKB MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP4TWM2OD16LkO0NFUzKM7:TR?= NFLDdldUSU6JRWK=
SCC-15 NXG3dVNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmftTWM2OD1zMD63O|g5KM7:TR?= NWroSoVXW0GQR1XS
BB49-HNC NWezNYxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXFVlZ6UUN3ME2xOE4{OzN3IN88US=> NEfxeY1USU6JRWK=
ES7 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1n3PWlEPTB;MUSuO|M4QSEQvF2= NVywW2ZOW0GQR1XS
LB2518-MEL MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjBSotwUUN3ME2xOk43ODl2IN88US=> NHvTOo1USU6JRWK=
NCI-H510A MnvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDBTWM2OD1zNz6yOFQzKM7:TR?= MYLTRW5ITVJ?
TE-441-T MnTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ZfmlEPTB;MUeuNlg5PiEQvF2= M1PvW3NCVkeHUh?=
HH NFfH[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF5LkO5PVkh|ryP M4e4bXNCVkeHUh?=
LC4-1 M4\sVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X2WmlEPTB;MUiuNFY2OiEQvF2= NF63dlhUSU6JRWK=
KARPAS-45 NY\1RmhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG1Z5VKUUN3ME2xPE4yQDR6IN88US=> M4jPSnNCVkeHUh?=
LB1047-RCC MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{X0NGlEPTB;MUiuOFQ2OiEQvF2= NG[4dXdUSU6JRWK=
NKM-1 NW\TdndCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHhbnV7UUN3ME2xPU4{PTV{IN88US=> NHLL[2JUSU6JRWK=
SCLC-21H MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmroTWM2OD1{MD6xNlQ3KM7:TR?= NEKzfZVUSU6JRWK=
RS4-11 NH60PXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nUcWlEPTB;MkCuN|MxQCEQvF2= NEftTmJUSU6JRWK=
ALL-PO MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlmxTWM2OD1{MD64NVQ6KM7:TR?= NWDLRVZCW0GQR1XS
GDM-1 NE\mUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDFR3VrUUN3ME2yNk42QTR3IN88US=> NWrQV4NkW0GQR1XS
DMS-79 NWXpcXNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn0bYdKSzVyPUK0MlQ6OzRizszN MXXTRW5ITVJ?
MPP-89 NY[0WGtHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rabWlEPTB;MkWuOlg4PCEQvF2= MYPTRW5ITVJ?
NB10 NUnnOW1KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTJ4LkS2PVkh|ryP MnjXV2FPT0WU
LS-513 NGLJWYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJ4Lki4OFch|ryP NHHkUIdUSU6JRWK=
L-540 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;JTWM2OD1{Nj65NVQ{KM7:TR?= NH7oSmZUSU6JRWK=
ES1 NFXi[IRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33MNmlEPTB;MkeuOVIyKM7:TR?= NWO1SVRnW0GQR1XS
NTERA-S-cl-D1 MmSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlm5TWM2OD1|MD61NFk{KM7:TR?= MVjTRW5ITVJ?
EW-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN{Lkm0OVQh|ryP MmHEV2FPT0WU
Calu-6 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[wT4tMUUN3ME2zN{4yQDV3IN88US=> NUHhfHBEW0GQR1XS
CTV-1 NYrneHNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTN|Lkm3PFkh|ryP MUDTRW5ITVJ?
YT NWjDO2ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHJTmJKSzVyPUO4MlUzODlizszN NU\Db21YW0GQR1XS
TE-6 MnG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTPbXJzUUN3ME20NU4zPzl6IN88US=> MoPGV2FPT0WU
HT-144 MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYraUVlpUUN3ME20NU42PDh4IN88US=> M1jrOnNCVkeHUh?=
EW-13 NIjlXGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPCeWNKSzVyPUSyMlI4QTFizszN MXXTRW5ITVJ?
KALS-1 NFr4UJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HlcWlEPTB;NEOuNVMzQSEQvF2= M1zGPHNCVkeHUh?=
MOLT-16 Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HJTmlEPTB;NEWuNFc2OiEQvF2= MmH6V2FPT0WU
D-336MG NGDlZXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTKTWM2OD12NT65OVk6KM7:TR?= M{PiXXNCVkeHUh?=
TE-11 NWHuW|ZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7Dc3Z3UUN3ME20Ok43PTNizszN MWTTRW5ITVJ?
EB2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDKXolYUUN3ME20Ok43QTlizszN MWXTRW5ITVJ?
SK-N-DZ NEPtRWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvjTWM2OD12OD6wPVYyKM7:TR?= NEfPb5dUSU6JRWK=
SW684 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTR6LkK2PVUh|ryP Ml74V2FPT0WU
EW-18 NXyxVGNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTMTplKSzVyPUS4MlQ{QTVizszN Mk\KV2FPT0WU
RL95-2 NHrxUohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq1TWM2OD13MD6wO|Eh|ryP NYLlSZN[W0GQR1XS
CHP-126 M2XRNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrvTWM2OD13MD64PVA2KM7:TR?= M{\aRXNCVkeHUh?=
NCI-H1395 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPNcIlKSzVyPUWxMlc5OzVizszN NEX0[|VUSU6JRWK=
TE-15 M1TqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVizOJZ3UUN3ME21Nk4zPTV4IN88US=> NEfPenhUSU6JRWK=
ES4 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTV{Lkm3O|Uh|ryP NVvRdm92W0GQR1XS
TE-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1viVWlEPTB;NUOuPVQ2PSEQvF2= MV\TRW5ITVJ?
SIMA MkjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTV5LkOzNVEh|ryP MYLTRW5ITVJ?
LB647-SCLC NIHKSmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTZ2LkGxPFgh|ryP NYPadHJLW0GQR1XS
KY821 M1[wXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXuOpJbUUN3ME22OE4zPTV{IN88US=> NXXEN2dLW0GQR1XS
LC-2-ad Mlz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTZ3Lke2NFEh|ryP MVPTRW5ITVJ?
KP-N-RT-BM-1 M4XPfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHjTWM2OD14Nj62N|Y3KM7:TR?= NVHlZXJpW0GQR1XS
SW872 NFTrR2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\DTWM2OD14Nz60N|gzKM7:TR?= NV3tfot6W0GQR1XS
ES5 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTZ5Lk[5Olgh|ryP MlzRV2FPT0WU
SK-NEP-1 NF;6SYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj1epdrUUN3ME22PE4{QDB|IN88US=> MknYV2FPT0WU
RPMI-6666 NYDuZnVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX3TWM2OD15MT6wN|Ih|ryP MVTTRW5ITVJ?
UACC-812 NEfrfnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHjTWM2OD15MT6xOlA6KM7:TR?= NUPJcG9mW0GQR1XS
COLO-829 NYLsR2pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\GTWM2OD15Mj62PVg4KM7:TR?= M1jVSHNCVkeHUh?=
KP-N-YS M2LaXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTd{LkexN|kh|ryP NIjZSnNUSU6JRWK=
GI-1 NV;ubmZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\zVGJVUUN3ME23N{4zQDZ6IN88US=> MknsV2FPT0WU
ETK-1 MkW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTd|LkS5N|Ih|ryP M4HwNHNCVkeHUh?=
LXF-289 NH7DTFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjVcItKSzVyPUezMlczQSEQvF2= MmDPV2FPT0WU
CAS-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33S[WlEPTB;N{OuPFg2PyEQvF2= MXTTRW5ITVJ?
EW-22 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mki3TWM2OD15ND63NVE2KM7:TR?= NUTxb2xFW0GQR1XS
NCI-H2196 NXHBd5NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPCTWM2OD15NT62N|c6KM7:TR?= NVPKSIViW0GQR1XS
EoL-1-cell NXvMV3gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRThzLk[5OlMh|ryP Mki4V2FPT0WU
D-247MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHkNm9KSzVyPUiyMlAzPDhizszN MmHHV2FPT0WU
Becker M1TwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7TdI5CUUN3ME24Nk4{PDhzIN88US=> MX3TRW5ITVJ?
IST-MEL1 MojzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXsOIZKSzVyPUiyMlM1QDJizszN NHTuTXRUSU6JRWK=
MDA-MB-134-VI MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jGcmlEPTB;OEKuOVk6PiEQvF2= MUjTRW5ITVJ?
NCI-H1092 MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnDWFlKSzVyPUi0MlAyQTdizszN MX3TRW5ITVJ?
KINGS-1 NVO5PIFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfTNnl[UUN3ME24Ok4yPjF6IN88US=> NYH0NXNJW0GQR1XS
HCC2218 Ml72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTh4Lke5NVMh|ryP MWfTRW5ITVJ?
GI-ME-N M3rxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXkOJVkUUN3ME24O{44Pjl7IN88US=> M1zoOnNCVkeHUh?=
AM-38 M{jvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPjNXdKSzVyPUi4MlM6PTNizszN NGnGS|VUSU6JRWK=
KNS-42 MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLrTWM2OD16OT6xNFE5KM7:TR?= Mkm5V2FPT0WU
C8166 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrm[YJMUUN3ME24PU43OTJ3IN88US=> MnvQV2FPT0WU
Ramos-2G6-4C10 NGL0XmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDSS2ZoUUN3ME24PU45PzF7IN88US=> M2S3cXNCVkeHUh?=
CTB-1 NXTke4RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nLUmlEPTB;OUCuOlM2PyEQvF2= MkW1V2FPT0WU
HCE-4 M1\6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj3TWM2OD17MT6xN|M3KM7:TR?= MkftV2FPT0WU
NCI-H526 NF\oW2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSyfFF3UUN3ME25Nk41OTB|IN88US=> M{XjUXNCVkeHUh?=
ECC4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPuTWM2OD17ND6yOVU2KM7:TR?= MlvuV2FPT0WU
NCCIT MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPITWM2OD17NT6zNlkzKM7:TR?= Mo\rV2FPT0WU
MZ7-mel M3LqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTl3LkmwOEDPxE1? NWPsUmU2W0GQR1XS
COLO-684 NE\qNYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r3OWlEPTB;OU[uNlM5PSEQvF2= M4DFcnNCVkeHUh?=
SU-DHL-1 M3vUSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXy5Tm1DUUN3ME25Ok46QDR{IN88US=> NV\BRXdvW0GQR1XS
SF126 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPIU|dKSzVyPUm3MlUzOTdizszN Mn3FV2FPT0WU
NMC-G1 MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[0RmlxUUN3ME25PE41PTV2IN88US=> MXrTRW5ITVJ?
NB14 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\TeXBKSzVyPUm4MlkzODhizszN NHi4[G9USU6JRWK=
VA-ES-BJ M3fTdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;WTnlRUUN3ME25PU41ODV4IN88US=> NF2wb4VUSU6JRWK=

... 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]
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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 (g) = Concentration (mol/L) × Volume (L) × 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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* 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

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  • 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):
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Molecular Weight Calculator

Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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
NCT03862768 Not yet recruiting Gastrointestinal Stromal Tumors|Surgery Shanghai Zhongshan Hospital July 2019 Not Applicable
NCT03862768 Not yet recruiting Gastrointestinal Stromal Tumors|Surgery Shanghai Zhongshan Hospital July 2019 Not Applicable
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03802084 Not yet recruiting Desmoid Tumor Yonsei University April 2019 Phase 1|Phase 2
NCT03802084 Not yet recruiting Desmoid Tumor Yonsei University April 2019 Phase 1|Phase 2

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