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 v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.

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Cited by 33 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.

     

    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.

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 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 M1ixOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMEezNFQh|ryP M4e1T3NCVkeHUh?=
EM-2 M3zyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O1TGlEPTB;MD6wPFg5KM7:TR?= NWTDTXpKW0GQR1XS
MEG-01 NID4fFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTBwMEi5NlEh|ryP MVHTRW5ITVJ?
BV-173 NF[yUIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\r[GlEPTB;MD6xPFc1KM7:TR?= NULwZZVtW0GQR1XS
K-562 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LZRWlEPTB;MD6yNlQ{OiEQvF2= NHS0R4NUSU6JRWK=
CGTH-W-1 MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTBwM{izO|Qh|ryP NH7QWVFUSU6JRWK=
ST486 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD3SHJwUUN3ME2wMlY5PTRizszN NUXZZY5EW0GQR1XS
NCI-H1436 NVjjN4RrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ny[mlEPTB;MD65O|gxOSEQvF2= NYDw[pRNW0GQR1XS
NOS-1 M1XjbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\EcI9KSzVyPUGuOlU{QDNizszN NFTweZhUSU6JRWK=
A498 NV\peYdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjH[nhKSzVyPUKuOVczOjNizszN M3jVZXNCVkeHUh?=
BE-13 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvyTWM2OD1{Lk[yNVA3KM7:TR?= MYrTRW5ITVJ?
SUP-T1 NFrF[G5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTNwOEK5NFch|ryP NWr4PXZDW0GQR1XS
NCI-H1770 NH\5NoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30U4tKSzVyPUWuOVczPjJizszN NX;yPJlIW0GQR1XS
IMR-5 NWDmdWZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XBUWlEPTB;Nj6yNlE1PyEQvF2= NX:wVpZlW0GQR1XS
LB2241-RCC MmO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml24TWM2OD16LkC3N|g1KM7:TR?= MXTTRW5ITVJ?
TGBC24TKB NVq2ZZFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHtOWJPUUN3ME24MlM1ODV{IN88US=> MX\TRW5ITVJ?
SCC-15 NUHSfI5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPz[4pKSzVyPUGwMlc4QDhizszN MX7TRW5ITVJ?
BB49-HNC NH64cVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO2bWd6UUN3ME2xOE4{OzN3IN88US=> NXnIc5hLW0GQR1XS
ES7 NEnneGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrTTWM2OD1zND63N|c6KM7:TR?= NVrCNXV3W0GQR1XS
LB2518-MEL M1;l[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvKR2NqUUN3ME2xOk43ODl2IN88US=> NWXwUYNlW0GQR1XS
NCI-H510A MlzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTF5LkK0OFIh|ryP M1TOVnNCVkeHUh?=
TE-441-T NHq1fHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;1WW9sUUN3ME2xO{4zQDh4IN88US=> MXvTRW5ITVJ?
HH NGmxXGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LxXWlEPTB;MUeuN|k6QSEQvF2= MmC2V2FPT0WU
LC4-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2H5W2lEPTB;MUiuNFY2OiEQvF2= M1HRb3NCVkeHUh?=
KARPAS-45 M1LL[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmriTWM2OD1zOD6xPFQ5KM7:TR?= MWjTRW5ITVJ?
LB1047-RCC NUXNfZhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDPXY5jUUN3ME2xPE41PDV{IN88US=> NXvPSoR6W0GQR1XS
NKM-1 NGjQc5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HFT2lEPTB;MUmuN|U2OiEQvF2= M17GU3NCVkeHUh?=
SCLC-21H NHr5cmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrINIZKSzVyPUKwMlEzPDZizszN MoCwV2FPT0WU
RS4-11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni3TWM2OD1{MD6zN|A5KM7:TR?= MXnTRW5ITVJ?
ALL-PO M3THO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3JU|hKSzVyPUKwMlgyPDlizszN Mli3V2FPT0WU
GDM-1 MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJ{LkW5OFUh|ryP NYDMZllRW0GQR1XS
DMS-79 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nYV2lEPTB;MkSuOFk{PCEQvF2= M4XVUnNCVkeHUh?=
MPP-89 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTJ3Lk[4O|Qh|ryP NGXmZpJUSU6JRWK=
NB10 NF3pZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJ4LkS2PVkh|ryP NVixRZV2W0GQR1XS
LS-513 NXPoS2k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTJ4Lki4OFch|ryP MWXTRW5ITVJ?
L-540 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HVUWlEPTB;Mk[uPVE1OyEQvF2= NISzTnhUSU6JRWK=
ES1 MlrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:5UFl3UUN3ME2yO{42OjFizszN NGjh[HJUSU6JRWK=
NTERA-S-cl-D1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrzTWM2OD1|MD61NFk{KM7:TR?= NUDwe3FSW0GQR1XS
EW-1 M2m5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrUTWM2OD1|Mj65OFU1KM7:TR?= MnTIV2FPT0WU
Calu-6 NInRTYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvCVFF{UUN3ME2zN{4yQDV3IN88US=> M33tcnNCVkeHUh?=
CTV-1 NEPlXFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVmxb5JNUUN3ME2zN{46Pzh7IN88US=> M4fWOHNCVkeHUh?=
YT NH[2SVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3VTWM2OD1|OD61NlA6KM7:TR?= NU\QUpY4W0GQR1XS
TE-6 NHPpO3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7qTWM2OD12MT6yO|k5KM7:TR?= M{jsV3NCVkeHUh?=
HT-144 NHT5Z2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTwTWM2OD12MT61OFg3KM7:TR?= MU\TRW5ITVJ?
EW-13 M4fTOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR{LkK3PVEh|ryP MnvGV2FPT0WU
KALS-1 NU[wXJFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\CWHBKSzVyPUSzMlE{OjlizszN NEnTbGNUSU6JRWK=
MOLT-16 M4\3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLnc4JHUUN3ME20OU4xPzV{IN88US=> NHe1b4JUSU6JRWK=
D-336MG M1\tbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LrRmlEPTB;NEWuPVU6QSEQvF2= M1LvRnNCVkeHUh?=
TE-11 NFywdmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\u[3pJUUN3ME20Ok43PTNizszN NX3u[o5UW0GQR1XS
EB2 NXPGNYhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;MRmlEPTB;NE[uOlk6KM7:TR?= MmrhV2FPT0WU
SK-N-DZ MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3SzOmlEPTB;NEiuNFk3OSEQvF2= NFG0R5RUSU6JRWK=
SW684 NYL0WGp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjleZlvUUN3ME20PE4zPjl3IN88US=> MmnFV2FPT0WU
EW-18 NYP5S|ZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KxNGlEPTB;NEiuOFM6PSEQvF2= NXy5[3p4W0GQR1XS
RL95-2 NHnZeo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnrNJBLUUN3ME21NE4xPzFizszN MUDTRW5ITVJ?
CHP-126 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;tW5pKSzVyPUWwMlg6ODVizszN M{XmcHNCVkeHUh?=
NCI-H1395 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDzTWM2OD13MT63PFM2KM7:TR?= MYPTRW5ITVJ?
TE-15 NYjWcYU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS2eW82UUN3ME21Nk4zPTV4IN88US=> NYXYSYFkW0GQR1XS
ES4 NULMV4Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYCyfmJCUUN3ME21Nk46Pzd3IN88US=> MYTTRW5ITVJ?
TE-1 M3Swe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3iyXWlEPTB;NUOuPVQ2PSEQvF2= MmDFV2FPT0WU
SIMA NYPRSpNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTV5LkOzNVEh|ryP NVXzU3Z{W0GQR1XS
LB647-SCLC MlPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jVXWlEPTB;NkSuNVE5QCEQvF2= MlvMV2FPT0WU
KY821 M4j2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTZ2LkK1OVIh|ryP NXyzR|ZHW0GQR1XS
LC-2-ad Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELpdWRKSzVyPU[1Mlc3ODFizszN M2T0WnNCVkeHUh?=
KP-N-RT-BM-1 NULuUotyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O3eWlEPTB;Nk[uOlM3PiEQvF2= MXnTRW5ITVJ?
SW872 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYOy[|N{UUN3ME22O{41Ozh{IN88US=> NV7MT2tGW0GQR1XS
ES5 Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fKSmlEPTB;NkeuOlk3QCEQvF2= Mn3CV2FPT0WU
SK-NEP-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPrNlI5UUN3ME22PE4{QDB|IN88US=> NVHXSXd1W0GQR1XS
RPMI-6666 MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LwWmlEPTB;N{GuNFMzKM7:TR?= MX\TRW5ITVJ?
UACC-812 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK4VHRKSzVyPUexMlE3ODlizszN NGXLSIdUSU6JRWK=
COLO-829 NVzndY9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTd{Lk[5PFch|ryP M{HMRnNCVkeHUh?=
KP-N-YS M1rB[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnCOVhoUUN3ME23Nk44OTN7IN88US=> MVLTRW5ITVJ?
GI-1 M3n5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\3W2lEPTB;N{OuNlg3QCEQvF2= M3PucHNCVkeHUh?=
ETK-1 NV;QclV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTd|LkS5N|Ih|ryP NGHNbYVUSU6JRWK=
LXF-289 NVvPNGxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[0d2lyUUN3ME23N{44OjlizszN Mn7NV2FPT0WU
CAS-1 NV;IdVdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jLcWlEPTB;N{OuPFg2PyEQvF2= NUWyPGt7W0GQR1XS
EW-22 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfEbFBLUUN3ME23OE44OTF3IN88US=> NHXHNlFUSU6JRWK=
NCI-H2196 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL0TWM2OD15NT62N|c6KM7:TR?= MX;TRW5ITVJ?
EoL-1-cell MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PX[mlEPTB;OEGuOlk3OyEQvF2= NGnIVpJUSU6JRWK=
D-247MG NVPJe5RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTh{LkCyOFgh|ryP NUHuUI1QW0GQR1XS
Becker NYHKZVJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnOTWM2OD16Mj6zOFgyKM7:TR?= MknZV2FPT0WU
IST-MEL1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUG1b|NiUUN3ME24Nk4{PDh{IN88US=> MnjyV2FPT0WU
MDA-MB-134-VI MmXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTh{LkW5PVYh|ryP MojtV2FPT0WU
NCI-H1092 NWPnVm43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjrbXJWUUN3ME24OE4xOTl5IN88US=> NHfTW3JUSU6JRWK=
KINGS-1 Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTh4LkG2NVgh|ryP Mo\VV2FPT0WU
HCC2218 M1nEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;QdWlEPTB;OE[uO|kyOyEQvF2= NGfOXZJUSU6JRWK=
GI-ME-N MmW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP2TWM2OD16Nz63Olk6KM7:TR?= NHzlWFRUSU6JRWK=
AM-38 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7tUJVKSzVyPUi4MlM6PTNizszN MlXOV2FPT0WU
KNS-42 M{X0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17sOmlEPTB;OEmuNVAyQCEQvF2= MoLiV2FPT0WU
C8166 NYTNUVRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfBdGlMUUN3ME24PU43OTJ3IN88US=> NIT0O5pUSU6JRWK=
Ramos-2G6-4C10 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle2TWM2OD16OT64O|E6KM7:TR?= NX\RS5dpW0GQR1XS
CTB-1 MnThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVuwVoZFUUN3ME25NE43OzV5IN88US=> NGHMOlhUSU6JRWK=
HCE-4 NIroc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHhbHpKSzVyPUmxMlE{OzZizszN MnfwV2FPT0WU
NCI-H526 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vGUWlEPTB;OUKuOFExOyEQvF2= MoftV2FPT0WU
ECC4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\BZmlEPTB;OUSuNlU2PSEQvF2= M1L2SHNCVkeHUh?=
NCCIT NEPtSXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTl3LkOyPVIh|ryP NYCwcpRHW0GQR1XS
MZ7-mel MoDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C4W2lEPTB;OUWuPVA1KM7:TR?= MYfTRW5ITVJ?
COLO-684 NHi3U2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvsSmVKSzVyPUm2MlI{QDVizszN MUPTRW5ITVJ?
SU-DHL-1 M3TXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\pTWM2OD17Nj65PFQzKM7:TR?= MmPNV2FPT0WU
SF126 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLyTWM2OD17Nz61NlE4KM7:TR?= MlrMV2FPT0WU
NMC-G1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTl6LkS1OVQh|ryP MkTuV2FPT0WU
NB14 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W2S2lEPTB;OUiuPVIxQCEQvF2= NGj4SZdUSU6JRWK=
VA-ES-BJ MmPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrZNJFKSzVyPUm5MlQxPTZizszN M{LYTHNCVkeHUh?=

... 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]
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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