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

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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.

    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 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwMEezNFQh|ryP M1LY[XNCVkeHUh?=
EM-2 MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml60TWM2OD1yLkC4PFgh|ryP NGrvXW9USU6JRWK=
MEG-01 NFmzbnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7LTWM2OD1yLkC4PVIyKM7:TR?= NXz6ToRlW0GQR1XS
BV-173 M1jTO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i2NmlEPTB;MD6xPFc1KM7:TR?= M1Pib3NCVkeHUh?=
K-562 NI\GfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjoTYpKSzVyPUCuNlI1OzJizszN NYHiSIRPW0GQR1XS
CGTH-W-1 NYPkfotKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwM{izO|Qh|ryP MWXTRW5ITVJ?
ST486 NWfsVndnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XjPWlEPTB;MD62PFU1KM7:TR?= NUjMNlNLW0GQR1XS
NCI-H1436 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTBwOUe4NFEh|ryP NUDYcm4xW0GQR1XS
NOS-1 NHXhTlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGWz[|NKSzVyPUGuOlU{QDNizszN MYHTRW5ITVJ?
A498 NXPQ[4c5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFKxUJVKSzVyPUKuOVczOjNizszN M1nVcXNCVkeHUh?=
BE-13 M2PWO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr0RmFKSzVyPUKuOlIyODZizszN M3fNOHNCVkeHUh?=
SUP-T1 MoryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXHPGE6UUN3ME2zMlgzQTB5IN88US=> NInOTnpUSU6JRWK=
NCI-H1770 NFnZOZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m5VGlEPTB;NT61O|I3OiEQvF2= NGXK[mtUSU6JRWK=
IMR-5 NEHJcZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHId2JKSzVyPU[uNlIyPDdizszN NUTo[HVvW0GQR1XS
LB2241-RCC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXhTWM2OD16LkC3N|g1KM7:TR?= NV7iVmRxW0GQR1XS
TGBC24TKB NWKwenBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzBTWM2OD16LkO0NFUzKM7:TR?= NX;1RY9yW0GQR1XS
SCC-15 MkDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:5NmlEPTB;MUCuO|c5QCEQvF2= Mn;nV2FPT0WU
BB49-HNC M3rD[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTF2LkOzN|Uh|ryP MUPTRW5ITVJ?
ES7 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoiwTWM2OD1zND63N|c6KM7:TR?= M4nRRXNCVkeHUh?=
LB2518-MEL MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF4Lk[wPVQh|ryP NVOwc4wzW0GQR1XS
NCI-H510A M1LXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF5LkK0OFIh|ryP NU\LfnBPW0GQR1XS
TE-441-T MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXDTWM2OD1zNz6yPFg3KM7:TR?= NYT4VmJCW0GQR1XS
HH M1vkeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\yfZVKSzVyPUG3MlM6QTlizszN M1\kXHNCVkeHUh?=
LC4-1 M1nKdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF6LkC2OVIh|ryP M2jMVHNCVkeHUh?=
KARPAS-45 M2HOdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j3UGlEPTB;MUiuNVg1QCEQvF2= Ml\RV2FPT0WU
LB1047-RCC Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL5TWM2OD1zOD60OFUzKM7:TR?= M3HN[HNCVkeHUh?=
NKM-1 M{TUeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF7LkO1OVIh|ryP MmryV2FPT0WU
SCLC-21H M37hR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPHO3hUUUN3ME2yNE4yOjR4IN88US=> M3[5cXNCVkeHUh?=
RS4-11 M3LTTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TLfWlEPTB;MkCuN|MxQCEQvF2= NELod41USU6JRWK=
ALL-PO MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJyLkixOFkh|ryP M3vHcHNCVkeHUh?=
GDM-1 M2K4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJ{LkW5OFUh|ryP M3:4SnNCVkeHUh?=
DMS-79 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJ2LkS5N|Qh|ryP Mo[4V2FPT0WU
MPP-89 NWK1NIZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJ3Lk[4O|Qh|ryP NImyPGRUSU6JRWK=
NB10 NFq4T25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJ4LkS2PVkh|ryP MU\TRW5ITVJ?
LS-513 MoHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzaTXlKSzVyPUK2Mlg5PDdizszN MX7TRW5ITVJ?
L-540 NXXseoU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zHbGlEPTB;Mk[uPVE1OyEQvF2= NGrMTZJUSU6JRWK=
ES1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvneVNKSzVyPUK3MlUzOSEQvF2= NI[yWGNUSU6JRWK=
NTERA-S-cl-D1 NGjscVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi2cJhKSzVyPUOwMlUxQTNizszN MV7TRW5ITVJ?
EW-1 NGHBVY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIWwSVJKSzVyPUOyMlk1PTRizszN Ml7oV2FPT0WU
Calu-6 MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHVUVVKSzVyPUOzMlE5PTVizszN MVHTRW5ITVJ?
CTV-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ToS2lEPTB;M{OuPVc5QSEQvF2= Mo\DV2FPT0WU
YT MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzqTWM2OD1|OD61NlA6KM7:TR?= MlrhV2FPT0WU
TE-6 M{L2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTRzLkK3PVgh|ryP NXvwfZBHW0GQR1XS
HT-144 NWKxSYIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTRzLkW0PFYh|ryP Mnu0V2FPT0WU
EW-13 NULpU4xyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTiPI5UUUN3ME20Nk4zPzlzIN88US=> MlLQV2FPT0WU
KALS-1 NETqVWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:3TWM2OD12Mz6xN|I6KM7:TR?= NV3ENlh2W0GQR1XS
MOLT-16 NY\WNYhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojOTWM2OD12NT6wO|UzKM7:TR?= NFn6[HFUSU6JRWK=
D-336MG NV;Pc5FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq1WJZ5UUN3ME20OU46PTl7IN88US=> NHniSmtUSU6JRWK=
TE-11 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\rSYlKSzVyPUS2MlY2OyEQvF2= MnPtV2FPT0WU
EB2 Mnr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR4Lk[5PUDPxE1? NH3ndJRUSU6JRWK=
SK-N-DZ MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;pZ2lEPTB;NEiuNFk3OSEQvF2= M1XFPHNCVkeHUh?=
SW684 NGTmd5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPwSotKSzVyPUS4MlI3QTVizszN NGPndlFUSU6JRWK=
EW-18 M4rMcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\kSWFKSzVyPUS4MlQ{QTVizszN NXnXUIk6W0GQR1XS
RL95-2 M{nZO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTVyLkC3NUDPxE1? MkPnV2FPT0WU
CHP-126 NHLy[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C0[WlEPTB;NUCuPFkxPSEQvF2= M3vKRnNCVkeHUh?=
NCI-H1395 NIjzbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTVzLke4N|Uh|ryP NVmzeFhoW0GQR1XS
TE-15 NWXkbIxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTV{LkK1OVYh|ryP MnjnV2FPT0WU
ES4 NXnjcXB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTQTWM2OD13Mj65O|c2KM7:TR?= M1;NSHNCVkeHUh?=
TE-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTV|Lkm0OVUh|ryP NIq3PXhUSU6JRWK=
SIMA NW\GOlBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTV5LkOzNVEh|ryP NVTVPGZ5W0GQR1XS
LB647-SCLC NE\rephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrETWM2OD14ND6xNVg5KM7:TR?= MULTRW5ITVJ?
KY821 NHfCO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWO2SYVpUUN3ME22OE4zPTV{IN88US=> MX3TRW5ITVJ?
LC-2-ad MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXCeGpKSzVyPU[1Mlc3ODFizszN NWDEPYtiW0GQR1XS
KP-N-RT-BM-1 M3r1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LYW2lEPTB;Nk[uOlM3PiEQvF2= M3T6enNCVkeHUh?=
SW872 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzMbmxKSzVyPU[3MlQ{QDJizszN NVvZZpljW0GQR1XS
ES5 NUn3RZMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi4No5KSzVyPU[3MlY6PjhizszN MVPTRW5ITVJ?
SK-NEP-1 NGHkfJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jicWlEPTB;NkiuN|gxOyEQvF2= MWPTRW5ITVJ?
RPMI-6666 NGPycG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;NW|ZKSzVyPUexMlA{OiEQvF2= NFL0ZY9USU6JRWK=
UACC-812 NXHHb2dbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:1dWlEPTB;N{GuNVYxQSEQvF2= MYXTRW5ITVJ?
COLO-829 NHfxSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTd{Lk[5PFch|ryP NYDoW3dVW0GQR1XS
KP-N-YS MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13N[mlEPTB;N{KuO|E{QSEQvF2= MknRV2FPT0WU
GI-1 M2jkSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PHOmlEPTB;N{OuNlg3QCEQvF2= M3L3NHNCVkeHUh?=
ETK-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2iybWlEPTB;N{OuOFk{OiEQvF2= MmXsV2FPT0WU
LXF-289 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[5PW9KSzVyPUezMlczQSEQvF2= NYfuVWw1W0GQR1XS
CAS-1 M{C4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTd|Lki4OVch|ryP M3L2cnNCVkeHUh?=
EW-22 NHPW[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTMTWM2OD15ND63NVE2KM7:TR?= M2TFbXNCVkeHUh?=
NCI-H2196 NYLQRVJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;MTWM2OD15NT62N|c6KM7:TR?= M4rZPHNCVkeHUh?=
EoL-1-cell NFjGWZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRThzLk[5OlMh|ryP MoPXV2FPT0WU
D-247MG NYDYZlJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHqS41KSzVyPUiyMlAzPDhizszN Ml;5V2FPT0WU
Becker M{fGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrte41UUUN3ME24Nk4{PDhzIN88US=> NXz2e|VXW0GQR1XS
IST-MEL1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPvTWM2OD16Mj6zOFgzKM7:TR?= MVTTRW5ITVJ?
MDA-MB-134-VI MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTh{LkW5PVYh|ryP NWHvN45WW0GQR1XS
NCI-H1092 M{XBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHzZVRHUUN3ME24OE4xOTl5IN88US=> M{XWXnNCVkeHUh?=
KINGS-1 NUnlT5hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;Kd4xKSzVyPUi2MlE3OThizszN NGG0RopUSU6JRWK=
HCC2218 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnrUJpzUUN3ME24Ok44QTF|IN88US=> NG\USGlUSU6JRWK=
GI-ME-N M4jZb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnpPINKSzVyPUi3Mlc3QTlizszN Mn7lV2FPT0WU
AM-38 NX\KVHJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLPTWM2OD16OD6zPVU{KM7:TR?= NUP0SXJwW0GQR1XS
KNS-42 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3kR5RKSzVyPUi5MlExOThizszN MnniV2FPT0WU
C8166 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfSOItKSzVyPUi5MlYyOjVizszN NUfQT443W0GQR1XS
Ramos-2G6-4C10 M2HNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\PPGlEPTB;OEmuPFcyQSEQvF2= MV\TRW5ITVJ?
CTB-1 M4nzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ni[2lEPTB;OUCuOlM2PyEQvF2= M1TXbXNCVkeHUh?=
HCE-4 NWLHRYNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrGfJhKSzVyPUmxMlE{OzZizszN NFvnVW9USU6JRWK=
NCI-H526 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTl{LkSxNFMh|ryP MXrTRW5ITVJ?
ECC4 M2fJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHsTWM2OD17ND6yOVU2KM7:TR?= MXTTRW5ITVJ?
NCCIT Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULLeox[UUN3ME25OU4{Ojl{IN88US=> M{fu[nNCVkeHUh?=
MZ7-mel M1\UOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L0bmlEPTB;OUWuPVA1KM7:TR?= MnTMV2FPT0WU
COLO-684 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTl4LkKzPFUh|ryP MUXTRW5ITVJ?
SU-DHL-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi1Ro5oUUN3ME25Ok46QDR{IN88US=> MUXTRW5ITVJ?
SF126 MlLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vIb2lEPTB;OUeuOVIyPyEQvF2= MV3TRW5ITVJ?
NMC-G1 NE[1fllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLyU3BOUUN3ME25PE41PTV2IN88US=> MlfMV2FPT0WU
NB14 NFTNUmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zDb2lEPTB;OUiuPVIxQCEQvF2= M3y0b3NCVkeHUh?=
VA-ES-BJ NYXMPYVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrVVYhKSzVyPUm5MlQxPTZizszN NWrESlhnW0GQR1XS

... 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
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
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
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