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 NGjlWlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrz[VFKSzVyPUCuNFc{ODRizszN NHj3ZZhUSU6JRWK=
EM-2 NXTtT4RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnvOlVFUUN3ME2wMlA5QDhizszN M1zHVnNCVkeHUh?=
MEG-01 NHr1eVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPsPYZKSzVyPUCuNFg6OjFizszN NF;mTHJUSU6JRWK=
BV-173 NIDrRmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LUZWlEPTB;MD6xPFc1KM7:TR?= MlrOV2FPT0WU
K-562 NXjJZW5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwMkK0N|Ih|ryP NVXvVphVW0GQR1XS
CGTH-W-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwM{izO|Qh|ryP MUjTRW5ITVJ?
ST486 MkXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HpUmlEPTB;MD62PFU1KM7:TR?= NInJTm1USU6JRWK=
NCI-H1436 NIruUY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Lz[GlEPTB;MD65O|gxOSEQvF2= NUf1cIdkW0GQR1XS
NOS-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFwNkWzPFMh|ryP MkDWV2FPT0WU
A498 Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEOyRnFKSzVyPUKuOVczOjNizszN M37lPXNCVkeHUh?=
BE-13 NXPWZ|ROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HMXmlEPTB;Mj62NlExPiEQvF2= MUjTRW5ITVJ?
SUP-T1 Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDVNnNOUUN3ME2zMlgzQTB5IN88US=> M4\Td3NCVkeHUh?=
NCI-H1770 M{DQN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDCVYFlUUN3ME21MlU4OjZ{IN88US=> NGDC[5lUSU6JRWK=
IMR-5 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M162fmlEPTB;Nj6yNlE1PyEQvF2= M4noOHNCVkeHUh?=
LB2241-RCC NW\JR5F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRThwMEezPFQh|ryP MnfpV2FPT0WU
TGBC24TKB MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRThwM{SwOVIh|ryP MljjV2FPT0WU
SCC-15 NI\OfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFyLke3PFgh|ryP M1rRd3NCVkeHUh?=
BB49-HNC NI[3dnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTF2LkOzN|Uh|ryP NYXhb3pjW0GQR1XS
ES7 NWOxPHZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnEUVlKSzVyPUG0Mlc{PzlizszN MnT5V2FPT0WU
LB2518-MEL M2XCUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3uTWM2OD1zNj62NFk1KM7:TR?= MY\TRW5ITVJ?
NCI-H510A Mmf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHlTWM2OD1zNz6yOFQzKM7:TR?= MVLTRW5ITVJ?
TE-441-T M1flSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LPSGlEPTB;MUeuNlg5PiEQvF2= NHH4eVhUSU6JRWK=
HH Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\4PWlEPTB;MUeuN|k6QSEQvF2= MmLaV2FPT0WU
LC4-1 NHi4Z5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF6LkC2OVIh|ryP NHnRWZpUSU6JRWK=
KARPAS-45 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTsOm1LUUN3ME2xPE4yQDR6IN88US=> MXnTRW5ITVJ?
LB1047-RCC M{W2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXaZVdmUUN3ME2xPE41PDV{IN88US=> NIjzdI1USU6JRWK=
NKM-1 NF;5O3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFraR5pKSzVyPUG5MlM2PTJizszN MlvuV2FPT0WU
SCLC-21H NVXJN4RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzWTWM2OD1{MD6xNlQ3KM7:TR?= NI\zXIJUSU6JRWK=
RS4-11 NXLn[I1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTWeHZHUUN3ME2yNE4{OzB6IN88US=> MX3TRW5ITVJ?
ALL-PO NIPUS2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJyLkixOFkh|ryP MmDDV2FPT0WU
GDM-1 NFnoc2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXzTWM2OD1{Mj61PVQ2KM7:TR?= M1PpS3NCVkeHUh?=
DMS-79 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTCdIRPUUN3ME2yOE41QTN2IN88US=> MV;TRW5ITVJ?
MPP-89 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXy3PHVkUUN3ME2yOU43QDd2IN88US=> M1Lid3NCVkeHUh?=
NB10 M4DXdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDIZ2tzUUN3ME2yOk41Pjl7IN88US=> M2DCenNCVkeHUh?=
LS-513 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnHTWM2OD1{Nj64PFQ4KM7:TR?= NYXEUYI2W0GQR1XS
L-540 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPPW5hKSzVyPUK2MlkyPDNizszN M{HtWnNCVkeHUh?=
ES1 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDoWWxKSzVyPUK3MlUzOSEQvF2= NXL3XlI{W0GQR1XS
NTERA-S-cl-D1 MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTNyLkWwPVMh|ryP MoLGV2FPT0WU
EW-1 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN{Lkm0OVQh|ryP M1XMfHNCVkeHUh?=
Calu-6 M1fUdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHYTWM2OD1|Mz6xPFU2KM7:TR?= M4rpVHNCVkeHUh?=
CTV-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHhZWlDUUN3ME2zN{46Pzh7IN88US=> M4\VbXNCVkeHUh?=
YT NVjkZmpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPwTWM2OD1|OD61NlA6KM7:TR?= MUDTRW5ITVJ?
TE-6 NI\tZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT4TWM2OD12MT6yO|k5KM7:TR?= NYX0bVk2W0GQR1XS
HT-144 NEG4enNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTRzLkW0PFYh|ryP NV\rSYdKW0GQR1XS
EW-13 M37JVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPXTWM2OD12Mj6yO|kyKM7:TR?= MW\TRW5ITVJ?
KALS-1 NFzpfWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHSW21KSzVyPUSzMlE{OjlizszN NYPGUJFjW0GQR1XS
MOLT-16 NV[wb2dZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDkTWM2OD12NT6wO|UzKM7:TR?= NFPQU3JUSU6JRWK=
D-336MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTR3Lkm1PVkh|ryP NEGwUHZUSU6JRWK=
TE-11 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T4RWlEPTB;NE[uOlU{KM7:TR?= NFOwWIxUSU6JRWK=
EB2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLBSZVIUUN3ME20Ok43QTlizszN MoDFV2FPT0WU
SK-N-DZ NWnYSmF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDXbFQyUUN3ME20PE4xQTZzIN88US=> Ml\3V2FPT0WU
SW684 NFPlc2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETqZ2hKSzVyPUS4MlI3QTVizszN NUjrZ3FpW0GQR1XS
EW-18 Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3WXIRsUUN3ME20PE41Ozl3IN88US=> MmH3V2FPT0WU
RL95-2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTVyLkC3NUDPxE1? NUD0VnF3W0GQR1XS
CHP-126 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPPTWM2OD13MD64PVA2KM7:TR?= MkTiV2FPT0WU
NCI-H1395 NWXPVoNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD0TWM2OD13MT63PFM2KM7:TR?= MY\TRW5ITVJ?
TE-15 NVvzfVRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\TfIJKSzVyPUWyMlI2PTZizszN M4nSVnNCVkeHUh?=
ES4 NIXUb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWCzSXNIUUN3ME21Nk46Pzd3IN88US=> Mkf3V2FPT0WU
TE-1 NEnSOWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfPPVdoUUN3ME21N{46PDV3IN88US=> NWPPZXBmW0GQR1XS
SIMA NEfXTYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTV5LkOzNVEh|ryP NXrs[3l4W0GQR1XS
LB647-SCLC NVflTIc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7yTWM2OD14ND6xNVg5KM7:TR?= MkDhV2FPT0WU
KY821 MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LlN2lEPTB;NkSuNlU2OiEQvF2= Mlj6V2FPT0WU
LC-2-ad MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvUXolxUUN3ME22OU44PjBzIN88US=> MVfTRW5ITVJ?
KP-N-RT-BM-1 NYDoe|F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXVXoRKSzVyPU[2MlY{PjZizszN MnjiV2FPT0WU
SW872 NIDnNnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInmSYpKSzVyPU[3MlQ{QDJizszN NYmz[|dyW0GQR1XS
ES5 NEHxeJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q2Z2lEPTB;NkeuOlk3QCEQvF2= M3zYTnNCVkeHUh?=
SK-NEP-1 MnTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTZ6LkO4NFMh|ryP NYrxeo1mW0GQR1XS
RPMI-6666 M1fMXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1T3bGlEPTB;N{GuNFMzKM7:TR?= MVrTRW5ITVJ?
UACC-812 MmLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\pNmlEPTB;N{GuNVYxQSEQvF2= NFTjbIVUSU6JRWK=
COLO-829 M3X5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HjbGlEPTB;N{KuOlk5PyEQvF2= NFzSfW1USU6JRWK=
KP-N-YS MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTd{LkexN|kh|ryP M3rBSnNCVkeHUh?=
GI-1 MmX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXWSINKSzVyPUezMlI5PjhizszN M2ezPHNCVkeHUh?=
ETK-1 NUL0[ZRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nSdGlEPTB;N{OuOFk{OiEQvF2= MkDOV2FPT0WU
LXF-289 M2O2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LaVmlEPTB;N{OuO|I6KM7:TR?= M1eybnNCVkeHUh?=
CAS-1 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PQcmlEPTB;N{OuPFg2PyEQvF2= NGDQPGlUSU6JRWK=
EW-22 NFnLbYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\3XmlEPTB;N{SuO|EyPSEQvF2= MYrTRW5ITVJ?
NCI-H2196 NXjCXIJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\xfmlEPTB;N{WuOlM4QSEQvF2= M4\MOXNCVkeHUh?=
EoL-1-cell MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\rTWM2OD16MT62PVY{KM7:TR?= MV\TRW5ITVJ?
D-247MG NFXQOZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ZTWM2OD16Mj6wNlQ5KM7:TR?= MXPTRW5ITVJ?
Becker NIHSSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXwUol[UUN3ME24Nk4{PDhzIN88US=> NHTvR3pUSU6JRWK=
IST-MEL1 MkHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXTTWM2OD16Mj6zOFgzKM7:TR?= NU\EOXZYW0GQR1XS
MDA-MB-134-VI NYnPWXJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7RTWM2OD16Mj61PVk3KM7:TR?= MYPTRW5ITVJ?
NCI-H1092 NX;WWVdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\YZoxKSzVyPUi0MlAyQTdizszN M4XzfXNCVkeHUh?=
KINGS-1 NWTBU4tJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPkTWM2OD16Nj6xOlE5KM7:TR?= MkDFV2FPT0WU
HCC2218 NV3ob3J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTh4Lke5NVMh|ryP M1LjOHNCVkeHUh?=
GI-ME-N MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTh5Lke2PVkh|ryP MnTzV2FPT0WU
AM-38 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rZUWlEPTB;OEiuN|k2OyEQvF2= MnP4V2FPT0WU
KNS-42 M3XPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHzNmFKSzVyPUi5MlExOThizszN M1TpN3NCVkeHUh?=
C8166 NV\oRYQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj5TWM2OD16OT62NVI2KM7:TR?= MULTRW5ITVJ?
Ramos-2G6-4C10 NGXzdpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTh7Lki3NVkh|ryP NVzBfXZZW0GQR1XS
CTB-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPWbWc5UUN3ME25NE43OzV5IN88US=> MnXGV2FPT0WU
HCE-4 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTlzLkGzN|Yh|ryP NXPHTWRKW0GQR1XS
NCI-H526 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml35TWM2OD17Mj60NVA{KM7:TR?= MY\TRW5ITVJ?
ECC4 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfGXmxFUUN3ME25OE4zPTV3IN88US=> NHW5NXFUSU6JRWK=
NCCIT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTl3LkOyPVIh|ryP NXnuboluW0GQR1XS
MZ7-mel MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoqzTWM2OD17NT65NFQh|ryP NV31PWx{W0GQR1XS
COLO-684 NF25VZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTl4LkKzPFUh|ryP MVvTRW5ITVJ?
SU-DHL-1 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;jTWM2OD17Nj65PFQzKM7:TR?= NVXHO|A2W0GQR1XS
SF126 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUn5UW1{UUN3ME25O{42OjF5IN88US=> NGCxRVdUSU6JRWK=
NMC-G1 MlTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jHTGlEPTB;OUiuOFU2PCEQvF2= NI\0XZJUSU6JRWK=
NB14 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnwdo1KSzVyPUm4MlkzODhizszN NYG1R|hKW0GQR1XS
VA-ES-BJ NHXWOVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonZTWM2OD17OT60NFU3KM7:TR?= MoHTV2FPT0WU

... 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 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)

  • 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
NCT03343600 Recruiting Patients Who Have Received Allo-HSCT National Taiwan University Hospital|Far Eastern Memorial Hospital|Tri-Service General Hospital|National Cheng-Kung University Hospital|Hualien Tzu Chi General Hospital November 9 2017 Phase 2
NCT01343173 Completed Chronic Myeloid Leukaemia University Hospital Bordeaux April 6 2011 Not Applicable
NCT02812693 Withdrawn Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma Joanne Jeter|National Cancer Institute (NCI)|Merck Ltd.|Ohio State University Comprehensive Cancer Center November 4 2016 Phase 1|Phase 2
NCT02461849 Recruiting Advanced Refractory Cancer Samsung Medical Center April 4 2014 Phase 2
NCT02644525 Not yet recruiting Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) December 31 2015 Phase 2
NCT00471497 Active not recruiting Myelogenous Leukemia Chronic Novartis Pharmaceuticals|Novartis July 31 2007 Phase 3

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