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 35 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 M3LteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\QUmlEPTB;MD6wO|MxPCEQvF2= M1fEXHNCVkeHUh?=
EM-2 M{DFcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTIOYlsUUN3ME2wMlA5QDhizszN MVzTRW5ITVJ?
MEG-01 M1jYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwMEi5NlEh|ryP MUnTRW5ITVJ?
BV-173 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\y[245UUN3ME2wMlE5PzRizszN M4nmOHNCVkeHUh?=
K-562 M1jZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjGTWM2OD1yLkKyOFMzKM7:TR?= MnjGV2FPT0WU
CGTH-W-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f6eGlEPTB;MD6zPFM4PCEQvF2= NYL6fGJ5W0GQR1XS
ST486 M1\1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHOTWM2OD1yLk[4OVQh|ryP NHrPb|hUSU6JRWK=
NCI-H1436 NFTHcm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwOUe4NFEh|ryP NEHJXoVUSU6JRWK=
NOS-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3T1N2lEPTB;MT62OVM5OyEQvF2= M3;DTnNCVkeHUh?=
A498 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\RV2lEPTB;Mj61O|IzOyEQvF2= NFfWPWpUSU6JRWK=
BE-13 NX;5NWZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTlV4ZKSzVyPUKuOlIyODZizszN MYPTRW5ITVJ?
SUP-T1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPXVIRKSzVyPUOuPFI6ODdizszN Mn;2V2FPT0WU
NCI-H1770 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPIeFRuUUN3ME21MlU4OjZ{IN88US=> NVj6cIc2W0GQR1XS
IMR-5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf0TWM2OD14LkKyNVQ4KM7:TR?= MmfKV2FPT0WU
LB2241-RCC NIjiWVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjmNFRYUUN3ME24MlA4Ozh2IN88US=> NXrCN485W0GQR1XS
TGBC24TKB M3LQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRThwM{SwOVIh|ryP NGrieZFUSU6JRWK=
SCC-15 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnwUW1VUUN3ME2xNE44Pzh6IN88US=> M3\zW3NCVkeHUh?=
BB49-HNC M{P4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvVTWM2OD1zND6zN|M2KM7:TR?= Mo\SV2FPT0WU
ES7 NVj4cHdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3zVGFKSzVyPUG0Mlc{PzlizszN NGPCOnNUSU6JRWK=
LB2518-MEL MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX33fGpmUUN3ME2xOk43ODl2IN88US=> NYHYR2JpW0GQR1XS
NCI-H510A NGPUVFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnJNYJKSzVyPUG3MlI1PDJizszN NFy3T4xUSU6JRWK=
TE-441-T NWfiR3B2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\0ZmRKSzVyPUG3MlI5QDZizszN MUfTRW5ITVJ?
HH NVPS[G9vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjHXFNKSzVyPUG3MlM6QTlizszN NF7mNVlUSU6JRWK=
LC4-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnDTWM2OD1zOD6wOlUzKM7:TR?= M1nMPXNCVkeHUh?=
KARPAS-45 NF3nU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjMVIVKSzVyPUG4MlE5PDhizszN NXzxWJRUW0GQR1XS
LB1047-RCC Mkn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF6LkS0OVIh|ryP NULuRpRmW0GQR1XS
NKM-1 NGDRSndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLYTWM2OD1zOT6zOVUzKM7:TR?= MnTOV2FPT0WU
SCLC-21H NIP0XIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELGd5BKSzVyPUKwMlEzPDZizszN MVrTRW5ITVJ?
RS4-11 NIfaU4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJyLkOzNFgh|ryP M1m0WHNCVkeHUh?=
ALL-PO M4LyOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLVTWM2OD1{MD64NVQ6KM7:TR?= Mn;JV2FPT0WU
GDM-1 NG\icItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\lfIRKSzVyPUKyMlU6PDVizszN MmfSV2FPT0WU
DMS-79 NE\tWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJ2LkS5N|Qh|ryP MVHTRW5ITVJ?
MPP-89 M1TVSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjmTWM2OD1{NT62PFc1KM7:TR?= Mm\uV2FPT0WU
NB10 M4jrXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJ4LkS2PVkh|ryP NUPhe3dRW0GQR1XS
LS-513 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHqTWM2OD1{Nj64PFQ4KM7:TR?= MUnTRW5ITVJ?
L-540 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJ4LkmxOFMh|ryP NFzreVdUSU6JRWK=
ES1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJ5LkWyNUDPxE1? M1\n[XNCVkeHUh?=
NTERA-S-cl-D1 NEW5W|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\WTWM2OD1|MD61NFk{KM7:TR?= MX;TRW5ITVJ?
EW-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7LeHdKSzVyPUOyMlk1PTRizszN NUWxWVhnW0GQR1XS
Calu-6 Mnv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTN|LkG4OVUh|ryP NGjXW4FUSU6JRWK=
CTV-1 NVTVNHh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\3TWM2OD1|Mz65O|g6KM7:TR?= NGnISFZUSU6JRWK=
YT M{G0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTN6LkWyNFkh|ryP NUf4RmF[W0GQR1XS
TE-6 NYTVZ3VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\rTWM2OD12MT6yO|k5KM7:TR?= MWjTRW5ITVJ?
HT-144 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm1R3ZKSzVyPUSxMlU1QDZizszN NVi0dI5PW0GQR1XS
EW-13 M3Syemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTR{LkK3PVEh|ryP MWHTRW5ITVJ?
KALS-1 M3nEeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR|LkGzNlkh|ryP NH\Pe49USU6JRWK=
MOLT-16 M4rQSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTDTWM2OD12NT6wO|UzKM7:TR?= NGjGSYRUSU6JRWK=
D-336MG MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz4TWJ3UUN3ME20OU46PTl7IN88US=> M{jPOXNCVkeHUh?=
TE-11 NX;nboNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHJTWM2OD12Nj62OVMh|ryP M3HQT3NCVkeHUh?=
EB2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTR4Lk[5PUDPxE1? MoewV2FPT0WU
SK-N-DZ NV3VSZlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED3S4VKSzVyPUS4MlA6PjFizszN MkfvV2FPT0WU
SW684 NGrBZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rXcmlEPTB;NEiuNlY6PSEQvF2= NF\Ib3dUSU6JRWK=
EW-18 MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DrUmlEPTB;NEiuOFM6PSEQvF2= M4X5OnNCVkeHUh?=
RL95-2 NEf6RYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe1[Vl{UUN3ME21NE4xPzFizszN M2HZ[nNCVkeHUh?=
CHP-126 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jPU2lEPTB;NUCuPFkxPSEQvF2= MlvTV2FPT0WU
NCI-H1395 M1K2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTVzLke4N|Uh|ryP NYrSd2pmW0GQR1XS
TE-15 M2PUXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjpdY95UUN3ME21Nk4zPTV4IN88US=> MofVV2FPT0WU
ES4 NXzrT|dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrHTWM2OD13Mj65O|c2KM7:TR?= MUnTRW5ITVJ?
TE-1 MoKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\LN5htUUN3ME21N{46PDV3IN88US=> NFr5R4VUSU6JRWK=
SIMA M{fHSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fmfGlEPTB;NUeuN|MyOSEQvF2= Mki3V2FPT0WU
LB647-SCLC NIDUXZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTZ2LkGxPFgh|ryP Mmq1V2FPT0WU
KY821 NEW5OG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4myb2lEPTB;NkSuNlU2OiEQvF2= M4SwZ3NCVkeHUh?=
LC-2-ad NGLNc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljhTWM2OD14NT63OlAyKM7:TR?= NFnRUY1USU6JRWK=
KP-N-RT-BM-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTZ4Lk[zOlYh|ryP M4WwTXNCVkeHUh?=
SW872 NEjzWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HrZmlEPTB;NkeuOFM5OiEQvF2= NWC1bIp2W0GQR1XS
ES5 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\hTWM2OD14Nz62PVY5KM7:TR?= NEDKZYxUSU6JRWK=
SK-NEP-1 NULOUI91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTDPGczUUN3ME22PE4{QDB|IN88US=> MX\TRW5ITVJ?
RPMI-6666 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP4TWM2OD15MT6wN|Ih|ryP M2TSdnNCVkeHUh?=
UACC-812 M2PuT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTdzLkG2NFkh|ryP NYXabIk6W0GQR1XS
COLO-829 M3zJNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTYfJg2UUN3ME23Nk43QTh5IN88US=> M3nh[HNCVkeHUh?=
KP-N-YS MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPyTmdKSzVyPUeyMlcyOzlizszN MnvMV2FPT0WU
GI-1 NXGxbVBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULlWmpIUUN3ME23N{4zQDZ6IN88US=> NHfu[VRUSU6JRWK=
ETK-1 NUGzbpZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzxZm5KSzVyPUezMlQ6OzJizszN NG\Db5RUSU6JRWK=
LXF-289 NH7qS3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Xu[2lEPTB;N{OuO|I6KM7:TR?= M4nHZnNCVkeHUh?=
CAS-1 MmLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXXTWM2OD15Mz64PFU4KM7:TR?= NXXYbG1UW0GQR1XS
EW-22 NX7lXotHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2iwcmlEPTB;N{SuO|EyPSEQvF2= MYHTRW5ITVJ?
NCI-H2196 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{mx[GlEPTB;N{WuOlM4QSEQvF2= NYXUSFBbW0GQR1XS
EoL-1-cell NGHGdFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYizV|VoUUN3ME24NU43QTZ|IN88US=> NIDEV|VUSU6JRWK=
D-247MG MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnFPY0zUUN3ME24Nk4xOjR6IN88US=> M1HzV3NCVkeHUh?=
Becker MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTh{LkO0PFEh|ryP MmrDV2FPT0WU
IST-MEL1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfQdoF6UUN3ME24Nk4{PDh{IN88US=> M{HJVXNCVkeHUh?=
MDA-MB-134-VI M2\3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnXN|ZoUUN3ME24Nk42QTl4IN88US=> M{D0R3NCVkeHUh?=
NCI-H1092 NHrXRZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;1TWM2OD16ND6wNVk4KM7:TR?= MnmzV2FPT0WU
KINGS-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTh4LkG2NVgh|ryP NYf4NG1sW0GQR1XS
HCC2218 NVz6Wm01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH4OWI1UUN3ME24Ok44QTF|IN88US=> NXjWNFc1W0GQR1XS
GI-ME-N M3Hhd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTh5Lke2PVkh|ryP NEnxWXhUSU6JRWK=
AM-38 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HBbGlEPTB;OEiuN|k2OyEQvF2= MWnTRW5ITVJ?
KNS-42 M1HaOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjEdG9oUUN3ME24PU4yODF6IN88US=> MVjTRW5ITVJ?
C8166 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH32dnJKSzVyPUi5MlYyOjVizszN MmLhV2FPT0WU
Ramos-2G6-4C10 M1juN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LvfmlEPTB;OEmuPFcyQSEQvF2= NIXQWppUSU6JRWK=
CTB-1 NWnaVlhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13KNGlEPTB;OUCuOlM2PyEQvF2= NELEV2NUSU6JRWK=
HCE-4 NHnNSnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\UO2xKSzVyPUmxMlE{OzZizszN M2fNPXNCVkeHUh?=
NCI-H526 NVXES3JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXhcFlnUUN3ME25Nk41OTB|IN88US=> MXTTRW5ITVJ?
ECC4 NH3DdpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jWc2lEPTB;OUSuNlU2PSEQvF2= NXPOZWZ7W0GQR1XS
NCCIT NV7rdZBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{G4cWlEPTB;OUWuN|I6OiEQvF2= Mn7zV2FPT0WU
MZ7-mel M1\NfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\uc45KSzVyPUm1MlkxPCEQvF2= M{jWe3NCVkeHUh?=
COLO-684 M1jKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rLVGlEPTB;OU[uNlM5PSEQvF2= MXvTRW5ITVJ?
SU-DHL-1 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz2T2xWUUN3ME25Ok46QDR{IN88US=> MofHV2FPT0WU
SF126 NWXEe4RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTl5LkWyNVch|ryP M3v3SXNCVkeHUh?=
NMC-G1 NWfBdZo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTl6LkS1OVQh|ryP NF[zb5lUSU6JRWK=
NB14 NFrWU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnRTWM2OD17OD65NlA5KM7:TR?= MlTTV2FPT0WU
VA-ES-BJ M{i2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXxcopXUUN3ME25PU41ODV4IN88US=> MVvTRW5ITVJ?

... 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]

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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 4 mg/mL (8.1 mM)
Water Insoluble
Ethanol 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
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
NCT00044304 Recruiting Hypereosinophilic Syndrome National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 22, 2002 Phase 2
NCT02644525 Not yet recruiting Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) December 21, 2015 Phase 2
NCT03007147 Not yet recruiting B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|BCR-ABL1 Fusion Protein Expression|Minimal Residual Disease|Philadelphia Chromosome Positive|T Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Childrens Oncology Group|National Cancer Institute (NCI) July 2017 Phase 3
NCT03023046 Not yet recruiting Adult Acute Lymphoblastic Leukemia|Adult Lymphoblastic Lymphoma|CD20 Positive|Philadelphia Chromosome Positive University of Washington|National Cancer Institute (NCI) February 2017 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) January 2017 Phase 2
NCT02924714 Recruiting Gastrointestinal Stromal Tumor Oslo University Hospital January 2017 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:

    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