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 Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HuWmlEPTB;MD6wO|MxPCEQvF2= NIrKZlFUSU6JRWK=
EM-2 MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rTRmlEPTB;MD6wPFg5KM7:TR?= NG[yRnhUSU6JRWK=
MEG-01 NXPMbGNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMEi5NlEh|ryP NVLaR21yW0GQR1XS
BV-173 MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnu3TWM2OD1yLkG4O|Qh|ryP M{T6W3NCVkeHUh?=
K-562 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwMkK0N|Ih|ryP NXnyR3RwW0GQR1XS
CGTH-W-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPCU3BJUUN3ME2wMlM5Ozd2IN88US=> Mof6V2FPT0WU
ST486 M1TBfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwNki1OEDPxE1? M{Oxb3NCVkeHUh?=
NCI-H1436 NYGwVVFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7RRVFKSzVyPUCuPVc5ODFizszN NHHlbJJUSU6JRWK=
NOS-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XPfGlEPTB;MT62OVM5OyEQvF2= MV\TRW5ITVJ?
A498 MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXewUWI6UUN3ME2yMlU4OjJ|IN88US=> NGX5cnZUSU6JRWK=
BE-13 NFPwbpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjxR3BPUUN3ME2yMlYzOTB4IN88US=> NHL4R|RUSU6JRWK=
SUP-T1 MknRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn22TWM2OD1|LkiyPVA4KM7:TR?= MkS5V2FPT0WU
NCI-H1770 NEWze41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDMVZJKSzVyPUWuOVczPjJizszN MVzTRW5ITVJ?
IMR-5 MlyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jSO2lEPTB;Nj6yNlE1PyEQvF2= M1zzWnNCVkeHUh?=
LB2241-RCC M3jyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoraTWM2OD16LkC3N|g1KM7:TR?= M37ifHNCVkeHUh?=
TGBC24TKB M{\SO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;tTWM2OD16LkO0NFUzKM7:TR?= NHq0d5JUSU6JRWK=
SCC-15 NIf5ZYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLofXBKSzVyPUGwMlc4QDhizszN NEjZbXBUSU6JRWK=
BB49-HNC NHuz[m5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jnRWlEPTB;MUSuN|M{PSEQvF2= M{fnVXNCVkeHUh?=
ES7 NYPvW5lzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTF2LkezO|kh|ryP MlLhV2FPT0WU
LB2518-MEL NFHmeZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF4Lk[wPVQh|ryP Mm\5V2FPT0WU
NCI-H510A NGLDOWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rlUmlEPTB;MUeuNlQ1OiEQvF2= NUTXR4F5W0GQR1XS
TE-441-T NEjWW4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF5LkK4PFYh|ryP MYLTRW5ITVJ?
HH MkW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFey[VNKSzVyPUG3MlM6QTlizszN NXXyZll2W0GQR1XS
LC4-1 NV;UZYdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3W[VZUUUN3ME2xPE4xPjV{IN88US=> MlvZV2FPT0WU
KARPAS-45 NETtcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPtc2ZKSzVyPUG4MlE5PDhizszN M{TRNnNCVkeHUh?=
LB1047-RCC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TsRmlEPTB;MUiuOFQ2OiEQvF2= NVjHWY9MW0GQR1XS
NKM-1 M3H0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF7LkO1OVIh|ryP M2X6OnNCVkeHUh?=
SCLC-21H M2exW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvnTWM2OD1{MD6xNlQ3KM7:TR?= NH\ISHRUSU6JRWK=
RS4-11 NE\MW2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4WzbWlEPTB;MkCuN|MxQCEQvF2= MkjzV2FPT0WU
ALL-PO NXPlVXBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP2TWM2OD1{MD64NVQ6KM7:TR?= MVHTRW5ITVJ?
GDM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTJ{LkW5OFUh|ryP M{C5XnNCVkeHUh?=
DMS-79 M1fISGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTJ2LkS5N|Qh|ryP MX;TRW5ITVJ?
MPP-89 NHThUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofCTWM2OD1{NT62PFc1KM7:TR?= MnfiV2FPT0WU
NB10 M3HHeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[0SnBKSzVyPUK2MlQ3QTlizszN MVLTRW5ITVJ?
LS-513 NYTFfIE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTEW3dKSzVyPUK2Mlg5PDdizszN MkXtV2FPT0WU
L-540 Mo\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEixdGhKSzVyPUK2MlkyPDNizszN MYHTRW5ITVJ?
ES1 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;HTWM2OD1{Nz61NlEh|ryP M3j3PXNCVkeHUh?=
NTERA-S-cl-D1 MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3f4U2lEPTB;M{CuOVA6OyEQvF2= NHL4RZlUSU6JRWK=
EW-1 MlLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTN{Lkm0OVQh|ryP NGnFU2tUSU6JRWK=
Calu-6 NVfiUmkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHHTWM2OD1|Mz6xPFU2KM7:TR?= MlvCV2FPT0WU
CTV-1 MmjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInkPJpKSzVyPUOzMlk4QDlizszN M{nSRXNCVkeHUh?=
YT NFr0W4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTN6LkWyNFkh|ryP Mn7OV2FPT0WU
TE-6 NX[5Vo1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTRzLkK3PVgh|ryP NFHncVdUSU6JRWK=
HT-144 MmixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnsTWM2OD12MT61OFg3KM7:TR?= MnHrV2FPT0WU
EW-13 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXrd5B2UUN3ME20Nk4zPzlzIN88US=> MnnRV2FPT0WU
KALS-1 NEHSWodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTR|LkGzNlkh|ryP MmOzV2FPT0WU
MOLT-16 NETvUYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTR3LkC3OVIh|ryP M4m2PXNCVkeHUh?=
D-336MG MmLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HpXWlEPTB;NEWuPVU6QSEQvF2= NFXVZoFUSU6JRWK=
TE-11 MnOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTOSWJ2UUN3ME20Ok43PTNizszN MknOV2FPT0WU
EB2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK5RZRKSzVyPUS2MlY6QSEQvF2= M2XpO3NCVkeHUh?=
SK-N-DZ MoThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR6LkC5OlEh|ryP NV3L[oYxW0GQR1XS
SW684 NVixXpg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjoXFBkUUN3ME20PE4zPjl3IN88US=> MYXTRW5ITVJ?
EW-18 NVPPUYZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfHTWM2OD12OD60N|k2KM7:TR?= NF\kVlRUSU6JRWK=
RL95-2 MofKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLjO2V2UUN3ME21NE4xPzFizszN MXLTRW5ITVJ?
CHP-126 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVyLki5NFUh|ryP M3K2V3NCVkeHUh?=
NCI-H1395 NVLYZW1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVeyWlh6UUN3ME21NU44QDN3IN88US=> MWfTRW5ITVJ?
TE-15 NFPKOWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DzVGlEPTB;NUKuNlU2PiEQvF2= NUDWOY96W0GQR1XS
ES4 Mlm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTV{Lkm3O|Uh|ryP MXvTRW5ITVJ?
TE-1 MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTV|Lkm0OVUh|ryP MlLOV2FPT0WU
SIMA Mo\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TOe2lEPTB;NUeuN|MyOSEQvF2= NIDNS3FUSU6JRWK=
LB647-SCLC NHLldWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnrbYJKSzVyPU[0MlEyQDhizszN MljTV2FPT0WU
KY821 MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml73TWM2OD14ND6yOVUzKM7:TR?= M131TnNCVkeHUh?=
LC-2-ad MkT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHaTWM2OD14NT63OlAyKM7:TR?= NGnGeVNUSU6JRWK=
KP-N-RT-BM-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTZ4Lk[zOlYh|ryP NGnqOXNUSU6JRWK=
SW872 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTxTWM2OD14Nz60N|gzKM7:TR?= MUfTRW5ITVJ?
ES5 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S0U2lEPTB;NkeuOlk3QCEQvF2= Mk\GV2FPT0WU
SK-NEP-1 M4PPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIf4PYVKSzVyPU[4MlM5ODNizszN NV\xblNCW0GQR1XS
RPMI-6666 M2nQdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfKVXNSUUN3ME23NU4xOzJizszN NH:2VYlUSU6JRWK=
UACC-812 NFfsd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTTWpVPUUN3ME23NU4yPjB7IN88US=> MWXTRW5ITVJ?
COLO-829 NH3X[nRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\oOmlEPTB;N{KuOlk5PyEQvF2= M3XwSHNCVkeHUh?=
KP-N-YS M4jnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm5eolKSzVyPUeyMlcyOzlizszN M1;WbXNCVkeHUh?=
GI-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DHZmlEPTB;N{OuNlg3QCEQvF2= MWrTRW5ITVJ?
ETK-1 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrLTWM2OD15Mz60PVMzKM7:TR?= NXz6dVNWW0GQR1XS
LXF-289 M2iyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XGdWlEPTB;N{OuO|I6KM7:TR?= M1j1TXNCVkeHUh?=
CAS-1 MmHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX4dY1jUUN3ME23N{45QDV5IN88US=> NWHiNWRyW0GQR1XS
EW-22 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTd2LkexNVUh|ryP NVm1RWN2W0GQR1XS
NCI-H2196 M3fSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTd3Lk[zO|kh|ryP M4OxNnNCVkeHUh?=
EoL-1-cell MnHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPCTWM2OD16MT62PVY{KM7:TR?= MXjTRW5ITVJ?
D-247MG MoDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\6botKSzVyPUiyMlAzPDhizszN M4PPNXNCVkeHUh?=
Becker NV7ud2d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELQW5RKSzVyPUiyMlM1QDFizszN NGX4fIxUSU6JRWK=
IST-MEL1 NV;JdIRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrnT|RKSzVyPUiyMlM1QDJizszN MUnTRW5ITVJ?
MDA-MB-134-VI MkS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\xVo5KSzVyPUiyMlU6QTZizszN M1Tn[nNCVkeHUh?=
NCI-H1092 M3XsbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPwTWM2OD16ND6wNVk4KM7:TR?= MWjTRW5ITVJ?
KINGS-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWexXYdLUUN3ME24Ok4yPjF6IN88US=> MorzV2FPT0WU
HCC2218 M{[w[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDaRnpKSzVyPUi2Mlc6OTNizszN Ml\FV2FPT0WU
GI-ME-N MlPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHJTWM2OD16Nz63Olk6KM7:TR?= NWryXVM4W0GQR1XS
AM-38 NV7lS2N5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH5TWM2OD16OD6zPVU{KM7:TR?= NELWc4dUSU6JRWK=
KNS-42 M1zqTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zvTGlEPTB;OEmuNVAyQCEQvF2= MWTTRW5ITVJ?
C8166 NYXTc3R1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P1cmlEPTB;OEmuOlEzPSEQvF2= NYHnfFVkW0GQR1XS
Ramos-2G6-4C10 NWC3O5dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjBOJhKSzVyPUi5Mlg4OTlizszN MmTEV2FPT0WU
CTB-1 MkS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X4TmlEPTB;OUCuOlM2PyEQvF2= MYfTRW5ITVJ?
HCE-4 NYmxd3FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7nTWM2OD17MT6xN|M3KM7:TR?= MkHPV2FPT0WU
NCI-H526 NXe3OWVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LxZWlEPTB;OUKuOFExOyEQvF2= NGi5R3VUSU6JRWK=
ECC4 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInxVXRKSzVyPUm0MlI2PTVizszN MmTMV2FPT0WU
NCCIT MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\wZ5FKSzVyPUm1MlMzQTJizszN Mkj4V2FPT0WU
MZ7-mel NX;EV5NUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLlOXZKSzVyPUm1MlkxPCEQvF2= MnGxV2FPT0WU
COLO-684 MmnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPETWM2OD17Nj6yN|g2KM7:TR?= M1;Re3NCVkeHUh?=
SU-DHL-1 NULIOlM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LyemlEPTB;OU[uPVg1OiEQvF2= M4rGRnNCVkeHUh?=
SF126 M2XuUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HaSmlEPTB;OUeuOVIyPyEQvF2= NUHXS2dwW0GQR1XS
NMC-G1 M4LVSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vQdGlEPTB;OUiuOFU2PCEQvF2= M3;4NHNCVkeHUh?=
NB14 NGC2Zo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTl6LkmyNFgh|ryP NWrF[VZnW0GQR1XS
VA-ES-BJ M2DTfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[5TWM2OD17OT60NFU3KM7:TR?= MnvsV2FPT0WU

... 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:

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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
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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID