Imatinib (STI571)

For research use only.

Catalog No.S2475 Synonyms: CGP057148B, ST-1571

154 publications

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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Selleck's Imatinib (STI571) has been cited by 154 publications

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 NWrp[ndCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwMEezNFQh|ryP M1Tx[XNCVkeHUh?=
EM-2 MlO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjY[YxKSzVyPUCuNFg5QCEQvF2= MUDTRW5ITVJ?
MEG-01 M1XRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwMEi5NlEh|ryP NVXEPYdtW0GQR1XS
BV-173 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwMUi3OEDPxE1? NUmzVWFKW0GQR1XS
K-562 NWT3cFlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;2O29KSzVyPUCuNlI1OzJizszN NXHlT2ozW0GQR1XS
CGTH-W-1 NETBRpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;iO2lEPTB;MD6zPFM4PCEQvF2= MoS1V2FPT0WU
ST486 Mn3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwNki1OEDPxE1? NH\x[WZUSU6JRWK=
NCI-H1436 NGXPWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkKyTWM2OD1yLkm3PFAyKM7:TR?= M37oRnNCVkeHUh?=
NOS-1 MnryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFwNkWzPFMh|ryP NGPuWY5USU6JRWK=
A498 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\yTWM2OD1{LkW3NlI{KM7:TR?= M4PlPXNCVkeHUh?=
BE-13 M1;vXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFT4bpRKSzVyPUKuOlIyODZizszN NHf6OI9USU6JRWK=
SUP-T1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M372[WlEPTB;Mz64NlkxPyEQvF2= NHTIfGxUSU6JRWK=
NCI-H1770 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K3VGlEPTB;NT61O|I3OiEQvF2= NFz3cmlUSU6JRWK=
IMR-5 NWe5doFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzYTWM2OD14LkKyNVQ4KM7:TR?= MX;TRW5ITVJ?
LB2241-RCC M1jBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDHbpZsUUN3ME24MlA4Ozh2IN88US=> MnnZV2FPT0WU
TGBC24TKB MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPETWM2OD16LkO0NFUzKM7:TR?= M4PvN3NCVkeHUh?=
SCC-15 NH7JNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnQT5RKSzVyPUGwMlc4QDhizszN NVzX[VhtW0GQR1XS
BB49-HNC Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF2LkOzN|Uh|ryP NF;2[IdUSU6JRWK=
ES7 NHfwWG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13ZUWlEPTB;MUSuO|M4QSEQvF2= NVvDc|doW0GQR1XS
LB2518-MEL M2LiXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHz0d|NKSzVyPUG2MlYxQTRizszN MYXTRW5ITVJ?
NCI-H510A NXHNN41VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDnTJdoUUN3ME2xO{4zPDR{IN88US=> Mm\2V2FPT0WU
TE-441-T M1vzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjYV21KSzVyPUG3MlI5QDZizszN MonDV2FPT0WU
HH NIrodXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnBTWM2OD1zNz6zPVk6KM7:TR?= NVKyZm5UW0GQR1XS
LC4-1 MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoH3TWM2OD1zOD6wOlUzKM7:TR?= M2jZOHNCVkeHUh?=
KARPAS-45 NHrFOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LM[GlEPTB;MUiuNVg1QCEQvF2= NWHQVIZtW0GQR1XS
LB1047-RCC M3[4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF6LkS0OVIh|ryP MWPTRW5ITVJ?
NKM-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF7LkO1OVIh|ryP NHv4SmtUSU6JRWK=
SCLC-21H MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T4W2lEPTB;MkCuNVI1PiEQvF2= NGH5VolUSU6JRWK=
RS4-11 NXXrNHFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXTTWM2OD1{MD6zN|A5KM7:TR?= Mn\0V2FPT0WU
ALL-PO MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJyLkixOFkh|ryP NVTTdoVFW0GQR1XS
GDM-1 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ{LkW5OFUh|ryP NF\tVHlUSU6JRWK=
DMS-79 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXj1fXMxUUN3ME2yOE41QTN2IN88US=> NYO1UXExW0GQR1XS
MPP-89 NVTSXpM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJ3Lk[4O|Qh|ryP M2f4T3NCVkeHUh?=
NB10 NHrFUXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LjcGlEPTB;Mk[uOFY6QSEQvF2= M3mwNHNCVkeHUh?=
LS-513 NU\xcoxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzrfIxKSzVyPUK2Mlg5PDdizszN MXfTRW5ITVJ?
L-540 NFr5VVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXzVolKSzVyPUK2MlkyPDNizszN MmfCV2FPT0WU
ES1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLkTWM2OD1{Nz61NlEh|ryP NInFcVVUSU6JRWK=
NTERA-S-cl-D1 NIXUeHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\HbG1KSzVyPUOwMlUxQTNizszN NH7lO25USU6JRWK=
EW-1 M1XP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnexTWM2OD1|Mj65OFU1KM7:TR?= M2jSZ3NCVkeHUh?=
Calu-6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTSTWM2OD1|Mz6xPFU2KM7:TR?= MlXBV2FPT0WU
CTV-1 NYXlVHRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDoVXhTUUN3ME2zN{46Pzh7IN88US=> NHKx[VZUSU6JRWK=
YT NVTZdY9QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTN6LkWyNFkh|ryP NH64UJFUSU6JRWK=
TE-6 MofWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3oeVB5UUN3ME20NU4zPzl6IN88US=> NIfsSpRUSU6JRWK=
HT-144 NH7JfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnhVFRPUUN3ME20NU42PDh4IN88US=> MYLTRW5ITVJ?
EW-13 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqzTWM2OD12Mj6yO|kyKM7:TR?= MofXV2FPT0WU
KALS-1 NF;TWYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLPc3VxUUN3ME20N{4yOzJ7IN88US=> Mk[zV2FPT0WU
MOLT-16 NVvpbGJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHuTWM2OD12NT6wO|UzKM7:TR?= NVjxVVRrW0GQR1XS
D-336MG NV65SoliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrGSVFKSzVyPUS1Mlk2QTlizszN NYXsR5FIW0GQR1XS
TE-11 MmG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfVTWM2OD12Nj62OVMh|ryP M2DvdnNCVkeHUh?=
EB2 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTMTWM2OD12Nj62PVkh|ryP NXLzSo9wW0GQR1XS
SK-N-DZ M3\aSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjaTWM2OD12OD6wPVYyKM7:TR?= NWTzPGxlW0GQR1XS
SW684 MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFf2WZdKSzVyPUS4MlI3QTVizszN M1y0PHNCVkeHUh?=
EW-18 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17RR2lEPTB;NEiuOFM6PSEQvF2= MWDTRW5ITVJ?
RL95-2 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fZbWlEPTB;NUCuNFcyKM7:TR?= MnLqV2FPT0WU
CHP-126 NWPqNGpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfpXJJKSzVyPUWwMlg6ODVizszN NGHVZYlUSU6JRWK=
NCI-H1395 M3XOW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTVzLke4N|Uh|ryP NYXJVHBFW0GQR1XS
TE-15 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LyfGlEPTB;NUKuNlU2PiEQvF2= MXXTRW5ITVJ?
ES4 M2ftSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTV{Lkm3O|Uh|ryP M2fadHNCVkeHUh?=
TE-1 MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofBTWM2OD13Mz65OFU2KM7:TR?= MmDTV2FPT0WU
SIMA NEnmcXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTV5LkOzNVEh|ryP M{G3[XNCVkeHUh?=
LB647-SCLC NEez[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\hWGVRUUN3ME22OE4yOTh6IN88US=> NHK5d2NUSU6JRWK=
KY821 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjoTWM2OD14ND6yOVUzKM7:TR?= NXXDOVJmW0GQR1XS
LC-2-ad MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjOflFKSzVyPU[1Mlc3ODFizszN MYfTRW5ITVJ?
KP-N-RT-BM-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rhcGlEPTB;Nk[uOlM3PiEQvF2= NU\ncYlQW0GQR1XS
SW872 NEG0NY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoSwTWM2OD14Nz60N|gzKM7:TR?= Mn3lV2FPT0WU
ES5 NVHCOWJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfkTldiUUN3ME22O{43QTZ6IN88US=> MVvTRW5ITVJ?
SK-NEP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSxXVV2UUN3ME22PE4{QDB|IN88US=> Moq2V2FPT0WU
RPMI-6666 M2rYNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHqc45wUUN3ME23NU4xOzJizszN MkfaV2FPT0WU
UACC-812 NH:1bXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\0TWM2OD15MT6xOlA6KM7:TR?= NYq4NHhiW0GQR1XS
COLO-829 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\PVGlEPTB;N{KuOlk5PyEQvF2= NWHaeVZtW0GQR1XS
KP-N-YS M1nJZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHFPGhHUUN3ME23Nk44OTN7IN88US=> M4jJdHNCVkeHUh?=
GI-1 NIHhenZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\2WoF7UUN3ME23N{4zQDZ6IN88US=> M3PmTnNCVkeHUh?=
ETK-1 NITHR5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TWW2lEPTB;N{OuOFk{OiEQvF2= MojRV2FPT0WU
LXF-289 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHRV4pKSzVyPUezMlczQSEQvF2= NY\Ic3h7W0GQR1XS
CAS-1 NGDPPGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PReWlEPTB;N{OuPFg2PyEQvF2= NUfr[o5{W0GQR1XS
EW-22 MnvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrRcI1KSzVyPUe0MlcyOTVizszN M3nlZnNCVkeHUh?=
NCI-H2196 M{P1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXQO3RKSzVyPUe1MlY{PzlizszN MX7TRW5ITVJ?
EoL-1-cell NIDnb25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRThzLk[5OlMh|ryP NE\ac2pUSU6JRWK=
D-247MG NH7ibphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmyWm5sUUN3ME24Nk4xOjR6IN88US=> MWDTRW5ITVJ?
Becker NX7hSmV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TsbWlEPTB;OEKuN|Q5OSEQvF2= MnuwV2FPT0WU
IST-MEL1 Mn\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnYTWM2OD16Mj6zOFgzKM7:TR?= NHWzRZlUSU6JRWK=
MDA-MB-134-VI M{fzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILKdlZKSzVyPUiyMlU6QTZizszN MWjTRW5ITVJ?
NCI-H1092 NVPqVFdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL5UFRKSzVyPUi0MlAyQTdizszN NU\pO3hNW0GQR1XS
KINGS-1 NYfmT5JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTUcnc6UUN3ME24Ok4yPjF6IN88US=> NFTWZWNUSU6JRWK=
HCC2218 M4L1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[xW3BwUUN3ME24Ok44QTF|IN88US=> MlPGV2FPT0WU
GI-ME-N NVfTOoJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XYPWlEPTB;OEeuO|Y6QSEQvF2= M{TsR3NCVkeHUh?=
AM-38 M3TLV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rwU2lEPTB;OEiuN|k2OyEQvF2= M1;jTHNCVkeHUh?=
KNS-42 NXfCd3RET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTh7LkGwNVgh|ryP M{fUdnNCVkeHUh?=
C8166 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTh7Lk[xNlUh|ryP MkHVV2FPT0WU
Ramos-2G6-4C10 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTh7Lki3NVkh|ryP MV7TRW5ITVJ?
CTB-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jzdGlEPTB;OUCuOlM2PyEQvF2= Ml[xV2FPT0WU
HCE-4 NYTCUnE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7VSFVKSzVyPUmxMlE{OzZizszN Mke1V2FPT0WU
NCI-H526 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfHXVlKSzVyPUmyMlQyODNizszN NXv4bFFDW0GQR1XS
ECC4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTl2LkK1OVUh|ryP MWrTRW5ITVJ?
NCCIT M{jKWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEG1VXNKSzVyPUm1MlMzQTJizszN MkjVV2FPT0WU
MZ7-mel MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPGeXhKSzVyPUm1MlkxPCEQvF2= M1j5bHNCVkeHUh?=
COLO-684 M3HxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTl4LkKzPFUh|ryP M3rBd3NCVkeHUh?=
SU-DHL-1 M2qwTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPiTWM2OD17Nj65PFQzKM7:TR?= NHrLeWhUSU6JRWK=
SF126 M3vQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:yW2lEPTB;OUeuOVIyPyEQvF2= NXy1XW8zW0GQR1XS
NMC-G1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTl6LkS1OVQh|ryP Ml\HV2FPT0WU
NB14 NXX0VJZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLvV2xKSzVyPUm4MlkzODhizszN MU\TRW5ITVJ?
VA-ES-BJ NVLLTZd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTl7LkSwOVYh|ryP MnLiV2FPT0WU

... 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 CN1CCN(CC1)CC2=CC=C(C=C2)C(=O)NC3=CC=C(C)C(=C3)NC4=NC=CC(=N4)C5=CC=CN=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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

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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    Volume
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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 )

  • 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 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 --
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
NCT04357613 Not yet recruiting Drug: Experimental drug SARS Virus Versailles Hospital May 1 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
NCT02644525 Active not recruiting Drug: Imatinib Mesylate|Drug: Placebo Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) September 16 2019 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:

    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