Imatinib (STI571)

For research use only.

Catalog No.S2475 Synonyms: CGP057148B, ST-1571

172 publications

Imatinib (STI571) Chemical Structure

CAS No. 152459-95-5

Imatinib (STI571, CGP057148B, ST-1571) 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. Imatinib (STI571) induces autophagy.

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Selleck's Imatinib (STI571) has been cited by 172 publications

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Choose Selective PDGFR Inhibitors

Biological Activity

Description Imatinib (STI571, CGP057148B, ST-1571) 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. Imatinib (STI571) induces autophagy.
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 M1nP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMEezNFQh|ryP NF[wVGVUSU6JRWK=
EM-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjVfVhkUUN3ME2wMlA5QDhizszN NV7BOoszW0GQR1XS
MEG-01 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XXTWlEPTB;MD6wPFkzOSEQvF2= NYGxSpQ5W0GQR1XS
BV-173 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwMUi3OEDPxE1? NIHKUHhUSU6JRWK=
K-562 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwMkK0N|Ih|ryP MnjrV2FPT0WU
CGTH-W-1 NIfzSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnONJJZUUN3ME2wMlM5Ozd2IN88US=> M{DaSHNCVkeHUh?=
ST486 NVvtSYRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXGWHNpUUN3ME2wMlY5PTRizszN Ml7VV2FPT0WU
NCI-H1436 NIS1N4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHyW5k3UUN3ME2wMlk4QDBzIN88US=> NVewdndlW0GQR1XS
NOS-1 NGXsc|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jZNWlEPTB;MT62OVM5OyEQvF2= MUfTRW5ITVJ?
A498 M{nCW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4j0WmlEPTB;Mj61O|IzOyEQvF2= NEPsOI9USU6JRWK=
BE-13 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJwNkKxNFYh|ryP MV7TRW5ITVJ?
SUP-T1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPJeYxKSzVyPUOuPFI6ODdizszN M1rZ[XNCVkeHUh?=
NCI-H1770 M2H6bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfNTWM2OD13LkW3NlYzKM7:TR?= MlzsV2FPT0WU
IMR-5 M1\oSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnQcHNKSzVyPU[uNlIyPDdizszN MlHCV2FPT0WU
LB2241-RCC MmjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzK[GNJUUN3ME24MlA4Ozh2IN88US=> M1z4e3NCVkeHUh?=
TGBC24TKB NYiwS2pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDCd4FKSzVyPUiuN|QxPTJizszN NXe2PIVDW0GQR1XS
SCC-15 NGrNT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S2UmlEPTB;MUCuO|c5QCEQvF2= M{jxcnNCVkeHUh?=
BB49-HNC MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\u[o1KSzVyPUG0MlM{OzVizszN M{jQPHNCVkeHUh?=
ES7 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLuTWM2OD1zND63N|c6KM7:TR?= M1PVe3NCVkeHUh?=
LB2518-MEL MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVf5WodzUUN3ME2xOk43ODl2IN88US=> MmrsV2FPT0WU
NCI-H510A MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\aTWM2OD1zNz6yOFQzKM7:TR?= M1znOnNCVkeHUh?=
TE-441-T MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm0bnZKSzVyPUG3MlI5QDZizszN NE\q[YNUSU6JRWK=
HH NUH1R5d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjJTWM2OD1zNz6zPVk6KM7:TR?= MnfsV2FPT0WU
LC4-1 NFHlNFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37JPGlEPTB;MUiuNFY2OiEQvF2= M2[yUnNCVkeHUh?=
KARPAS-45 M3H6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[xU4hKSzVyPUG4MlE5PDhizszN NIDLe|RUSU6JRWK=
LB1047-RCC NWHkUHd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HXT2lEPTB;MUiuOFQ2OiEQvF2= Mn7UV2FPT0WU
NKM-1 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L3cWlEPTB;MUmuN|U2OiEQvF2= MoH4V2FPT0WU
SCLC-21H MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXZcoRKSzVyPUKwMlEzPDZizszN MXjTRW5ITVJ?
RS4-11 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnQeIV1UUN3ME2yNE4{OzB6IN88US=> M4n6NXNCVkeHUh?=
ALL-PO MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljCTWM2OD1{MD64NVQ6KM7:TR?= MYHTRW5ITVJ?
GDM-1 M{WxWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zudGlEPTB;MkKuOVk1PSEQvF2= MkDrV2FPT0WU
DMS-79 NFXiN|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJ2LkS5N|Qh|ryP NHvHXWxUSU6JRWK=
MPP-89 NFHCc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfqTWM2OD1{NT62PFc1KM7:TR?= M2fzSXNCVkeHUh?=
NB10 NXfIco5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrh[YdMUUN3ME2yOk41Pjl7IN88US=> NIP3dW9USU6JRWK=
LS-513 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTJ4Lki4OFch|ryP MVrTRW5ITVJ?
L-540 NH3uTVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XyNmlEPTB;Mk[uPVE1OyEQvF2= M33BdnNCVkeHUh?=
ES1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXFb3pKUUN3ME2yO{42OjFizszN M3nIW3NCVkeHUh?=
NTERA-S-cl-D1 NUW4dGZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nwN2lEPTB;M{CuOVA6OyEQvF2= NVmyXmxvW0GQR1XS
EW-1 M2izRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTN{Lkm0OVQh|ryP M3rabnNCVkeHUh?=
Calu-6 M4LGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTN|LkG4OVUh|ryP NFjX[nNUSU6JRWK=
CTV-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvXTWM2OD1|Mz65O|g6KM7:TR?= Ml\iV2FPT0WU
YT NGHXOWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXy2NZZqUUN3ME2zPE42OjB7IN88US=> MXfTRW5ITVJ?
TE-6 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnlRWtKSzVyPUSxMlI4QThizszN MW\TRW5ITVJ?
HT-144 M{PHWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHSTWM2OD12MT61OFg3KM7:TR?= MmW4V2FPT0WU
EW-13 NYPjcnBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DtTWlEPTB;NEKuNlc6OSEQvF2= M1nYSnNCVkeHUh?=
KALS-1 M{LRWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTR|LkGzNlkh|ryP NIXZZo5USU6JRWK=
MOLT-16 M{fyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\PN|Z3UUN3ME20OU4xPzV{IN88US=> MmPPV2FPT0WU
D-336MG MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LZRmlEPTB;NEWuPVU6QSEQvF2= M2rZW3NCVkeHUh?=
TE-11 NEPLTnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPZTWM2OD12Nj62OVMh|ryP MV7TRW5ITVJ?
EB2 NV3YWXNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrlPI5tUUN3ME20Ok43QTlizszN MnTwV2FPT0WU
SK-N-DZ MkfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7vTWM2OD12OD6wPVYyKM7:TR?= NXnnW5dMW0GQR1XS
SW684 MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnGzTWM2OD12OD6yOlk2KM7:TR?= MUPTRW5ITVJ?
EW-18 M{TEZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH1cJN5UUN3ME20PE41Ozl3IN88US=> NELj[lFUSU6JRWK=
RL95-2 NVTPOpNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjHXJpKSzVyPUWwMlA4OSEQvF2= NHzRRVZUSU6JRWK=
CHP-126 MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\OTWM2OD13MD64PVA2KM7:TR?= M2nXO3NCVkeHUh?=
NCI-H1395 NFzFOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzRTWM2OD13MT63PFM2KM7:TR?= NX3EcnhYW0GQR1XS
TE-15 MofwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTV{LkK1OVYh|ryP M1PUV3NCVkeHUh?=
ES4 NETibGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnFclJpUUN3ME21Nk46Pzd3IN88US=> MX\TRW5ITVJ?
TE-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPoSnJKSzVyPUWzMlk1PTVizszN NGfwfVdUSU6JRWK=
SIMA NU\1VGp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjYTY1KSzVyPUW3MlM{OTFizszN NI[5b|JUSU6JRWK=
LB647-SCLC NULUdXZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fFOWlEPTB;NkSuNVE5QCEQvF2= MnrhV2FPT0WU
KY821 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3QTWM2OD14ND6yOVUzKM7:TR?= M1\kfXNCVkeHUh?=
LC-2-ad M{GyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jqOWlEPTB;NkWuO|YxOSEQvF2= MmDuV2FPT0WU
KP-N-RT-BM-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnSc5ZKSzVyPU[2MlY{PjZizszN NY\kcFd3W0GQR1XS
SW872 M4LZZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HtOmlEPTB;NkeuOFM5OiEQvF2= NFz6c|RUSU6JRWK=
ES5 NXzH[YhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\2OFc{UUN3ME22O{43QTZ6IN88US=> MofjV2FPT0WU
SK-NEP-1 NEHY[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDqTWM2OD14OD6zPFA{KM7:TR?= NEnWbWpUSU6JRWK=
RPMI-6666 NV7zeHhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTdzLkCzNkDPxE1? NUG0fJVEW0GQR1XS
UACC-812 M3jOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTdzLkG2NFkh|ryP NVHQSmFqW0GQR1XS
COLO-829 NYDlTXpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm3WVlKSzVyPUeyMlY6QDdizszN M3Px[nNCVkeHUh?=
KP-N-YS NF3hTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf6VYFIUUN3ME23Nk44OTN7IN88US=> M4LzVnNCVkeHUh?=
GI-1 NGPRXFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUizTXFwUUN3ME23N{4zQDZ6IN88US=> NVzRT|JxW0GQR1XS
ETK-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X1TWlEPTB;N{OuOFk{OiEQvF2= NHf1PVVUSU6JRWK=
LXF-289 NHnmT4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\QeWxKSzVyPUezMlczQSEQvF2= M1\K[nNCVkeHUh?=
CAS-1 NWjOepdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\nVYJqUUN3ME23N{45QDV5IN88US=> Mm\JV2FPT0WU
EW-22 NV7PXXhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTd2LkexNVUh|ryP NU\Db3V2W0GQR1XS
NCI-H2196 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33Wc2lEPTB;N{WuOlM4QSEQvF2= Mom4V2FPT0WU
EoL-1-cell MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4KwWGlEPTB;OEGuOlk3OyEQvF2= M1HDcHNCVkeHUh?=
D-247MG MnnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXqwXG5XUUN3ME24Nk4xOjR6IN88US=> M4Lzc3NCVkeHUh?=
Becker M3n0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XBR2lEPTB;OEKuN|Q5OSEQvF2= NFKyTGRUSU6JRWK=
IST-MEL1 NXHj[Y5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXqeWo6UUN3ME24Nk4{PDh{IN88US=> NIrUS5dUSU6JRWK=
MDA-MB-134-VI M4rLfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HkTWlEPTB;OEKuOVk6PiEQvF2= NEj4OmdUSU6JRWK=
NCI-H1092 NWDIdW1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLGNol2UUN3ME24OE4xOTl5IN88US=> MVPTRW5ITVJ?
KINGS-1 MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTh4LkG2NVgh|ryP MoDmV2FPT0WU
HCC2218 Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvlTWM2OD16Nj63PVE{KM7:TR?= MkXFV2FPT0WU
GI-ME-N Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfxcHdKSzVyPUi3Mlc3QTlizszN MUjTRW5ITVJ?
AM-38 NV\l[XFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T5PWlEPTB;OEiuN|k2OyEQvF2= MojnV2FPT0WU
KNS-42 NUnmemlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK3TWM2OD16OT6xNFE5KM7:TR?= MoLjV2FPT0WU
C8166 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfENoNoUUN3ME24PU43OTJ3IN88US=> MofEV2FPT0WU
Ramos-2G6-4C10 NWO4OXRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\1R2lEPTB;OEmuPFcyQSEQvF2= M1fHSnNCVkeHUh?=
CTB-1 NXnlWVZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGKyblBKSzVyPUmwMlY{PTdizszN MX;TRW5ITVJ?
HCE-4 M1rzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;zTWlEPTB;OUGuNVM{PiEQvF2= MXjTRW5ITVJ?
NCI-H526 NVLqRZR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrYNYJKSzVyPUmyMlQyODNizszN NEXpNGpUSU6JRWK=
ECC4 M2fMWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zvVmlEPTB;OUSuNlU2PSEQvF2= MnjWV2FPT0WU
NCCIT Mk\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTl3LkOyPVIh|ryP M4TaZXNCVkeHUh?=
MZ7-mel M1\YWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDvbVI4UUN3ME25OU46ODRizszN MmXGV2FPT0WU
COLO-684 MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HIUGlEPTB;OU[uNlM5PSEQvF2= M16yPHNCVkeHUh?=
SU-DHL-1 NEHWV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf0SFBKSzVyPUm2Mlk5PDJizszN MULTRW5ITVJ?
SF126 M3fxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3pPYJLUUN3ME25O{42OjF5IN88US=> M3PEOHNCVkeHUh?=
NMC-G1 NWfZV3FwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH33VJBKSzVyPUm4MlQ2PTRizszN NWPwU|lFW0GQR1XS
NB14 MkLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;3OHRKSzVyPUm4MlkzODhizszN M4rXTHNCVkeHUh?=
VA-ES-BJ NHHOdGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTl7LkSwOVYh|ryP NE\rcplUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-STAT5 / STAT5 ; 

PubMed: 18981115     


For phospho-STAT3 and Phospho-STAT5 detection, cells were then activated for 6 hrs with anti-CD3 and anti-CD28 Ab. Equivalent amounts of protein from cell lysates were separated by SDS-PAGE and western blot analysis was then performed using anti-phospho STAT3, anti-STAT3, anti-phospho STAT5 or anti-STAT5 Abs.

p-ZAP70 / ZAP70 / p-LAT / LAT ; 

PubMed: 18981115     


For the analysis of imatinib interference with early TCR signaling events, cells were activated for 5 min with anti-CD3 and anti-CD28 Abs and blots were probed with anti-phospho ZAP70, anti-ZAP70, anti-phospho LAT or anti-LAT antibodies. Untreated, non-activated cells were used as controls (NA).

p-STAT3 / STAT3 / p-STAT5 / STAT5 ; 

PubMed: 18981115     


For phospho-STAT3 and Phospho-STAT5 detection, cells were then activated for 6 hrs with anti-CD3 and anti-CD28 Ab. Equivalent amounts of protein from cell lysates were separated by SDS-PAGE and western blot analysis was then performed using anti-phospho STAT3, anti-STAT3, anti-phospho STAT5 or anti-STAT5 Abs.

p-ZAP70 / ZAP70 / p-LAT / LAT ; 

PubMed: 18981115     


For the analysis of imatinib interference with early TCR signaling events, cells were activated for 5 min with anti-CD3 and anti-CD28 Abs and blots were probed with anti-phospho ZAP70, anti-ZAP70, anti-phospho LAT or anti-LAT antibodies. Untreated, non-activated cells were used as controls (NA).

18981115
Immunofluorescence
RelB; 

PubMed: 20371728     


Nuclear proteins were extracted from the untreated and treated cells and nuclear levels of RelA and RelB were confirmed by immunocytochemistry 

Cortactin / F-actin ; 

PubMed: 20937825     


NIH3T3-SrcY527F cells were treated with DMSO or with 10 μm STI571 for 16 h, fixed and co-stained for cortactin (red, left panels) and F-actin (green, middle panels). Merged fields (right panels) demonstrate co-localization between cortactin and F-actin at invadopodia.

RelB; 

PubMed: 20371728     


Nuclear proteins were extracted from the untreated and treated cells and nuclear levels of RelA and RelB were confirmed by immunocytochemistry.

Cortactin / F-actin ; 

PubMed: 20937825     


NIH3T3-SrcY527F cells were treated with DMSO or with 10 μm STI571 for 16 h, fixed and co-stained for cortactin (red, left panels) and F-actin (green, middle panels). Merged fields (right panels) demonstrate co-localization between cortactin and F-actin at invadopodia.

20371728 20937825
Growth inhibition assay
Cell viability ; 

PubMed: 28435223     


(C) K562 cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. (D) KBM7R cells were treated with imatinib (0–10 μM) alone or imatinib and BEZ235 (0.2 μM) for 48 h and subjected to MTS assay. Mean ± SD. n=3. *P<0.05, compared to the control group. #P<0.05, compared to the group of IM alone. Abbreviations: IM, imatinib; SD, standard deviation.

28435223
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)

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
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*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 )

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    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):
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    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:

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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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04326933 Not yet recruiting Drug: Tyrosine kinase Inhibitors (Imatinib & Nilotinib) Patients Diagnosed as Chronic Meyloid Leukemia Assiut University October 20 2020 --
NCT04357613 Not yet recruiting Drug: Experimental drug SARS Virus Versailles Hospital September 1 2020 Phase 2
NCT04422678 Not yet recruiting Drug: Imatinib Mesylate|Drug: Standard of Care COVID-19 Alexandria University|Science Technology & Innovation Funding Authority (STIFA) Egypt June 2020 Phase 3
NCT04097093 Not yet recruiting Other: No intervention GIST European Organisation for Research and Treatment of Cancer - EORTC June 1 2020 --
NCT03891901 Not yet recruiting Drug: Imatinib|Drug: Isoniazid|Drug: Rifabutin Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) June 2020 Phase 2
NCT03997903 Not yet recruiting Drug: Imatinib Mesylate Sickle Cell Disease Indiana University|Purdue University|Children''s Hospital Medical Center Cincinnati February 26 2020 Early Phase 1

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

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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