Imatinib (STI571) Mesylate

Catalog No.S1026 Synonyms: Gleevec, Glivec, CGP-57148B

For research use only.

Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which 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. Imatinib Mesylate (STI571) induces autophagy.

Imatinib (STI571) Mesylate Chemical Structure

CAS No. 220127-57-1

Selleck's Imatinib (STI571) Mesylate has been cited by 197 publications

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Biological Activity

Description Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which 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. Imatinib Mesylate (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
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K562 MlrIR5l1d3SxeHnjbZR6KEG|c3H5 NELVd3czPCCq MWrJR|UxRTBwMkGg{txO Ml;FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyMECyNFcoRjJ{MECwNlA4RC:jPh?=
MCF-7 NFrjUGREgXSxdH;4bYNqfHliQYPzZZk> M3TYOFI1KGh? NIfQb3FKSzVyPUCuPFMh|ryP MmfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyMECyNFcoRjJ{MECwNlA4RC:jPh?=
MDA-MB-23 MmjRR5l1d3SxeHnjbZR6KEG|c3H5 NFzGO5QzPCCq MYDJR|UxRTFwODFOwG0> NV7GZYd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwNFAzODdpPkKyNFAxOjB5PD;hQi=>
K562r NUHJWVFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP6TpVKSzVyPUGwxsDPxE1? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl|OUSxPEc,OjR7M{m0NVg9N2F-
K562 MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPFR|UxRTBwMEmg{txO MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ5OESxOEc,OTZ4N{i0NVQ9N2F-
MCF-7 NWTOfFh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3THbVExKM7:TR?= MXO0PEBp NYDRbGl2[myxY3vzJINmdGxicILvcIln\XKjdHnvckBqdmO{ZXHz[UBqdmS3Y3XkJIJ6KEKMM2q= MnnVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{SwN|QoRjJ3Mke0NFM1RC:jPh?=
K-562  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37G[2lEPTB;MTFOwG0> NHq2UmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKzPVY3Oid-MkWyN|k3PjJ:L3G+
K562  M4\1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDKeXRKSzVyPUCuOeKh|ryP MmfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7M{m0NVgoRjJ2OUO5OFE5RC:jPh?=
PC3  NF\2TIRCeG:ydH;zbZMhSXO|YYm= MWKyNQKBkc7:TR?= Mn70OFgwPzJiaB?= NUHIZmxJcW6lcnXhd4V{KGOnbHygd5Vzfmm4YXy= NYLG[3V5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PFY3PTZpPkK1O|g3PjV4PD;hQi=>
PC3  MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV:yNQKBkc7:TR?= NHK2flg3NTd{IHi= NYPwdnRqcW6lcnXhd4V{KGOnbHygeoli[mmuaYT5 NEn5NGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe4OlY2Pid-MkW3PFY3PTZ:L3G+
DU145 NGGxU3pCeG:ydH;zbZMhSXO|YYm= MWqyNQKBkc7:TR?= NInsXoM1QC95MjDo M{fjUYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCjcH;weI9{cXN? NXH0O3NCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PFY3PTZpPkK1O|g3PjV4PD;hQi=>
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Hep G2 NHzCXnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrSTWM2OD1|MTFOwG0> MmrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkOyN|IoRjJ3OE[zNlMzRC:jPh?=
T47D  MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfLVm9jUUN3ME21NEDPxE1? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4M{KzNkc,OjV6NkOyN|I9N2F-
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EOL-1 M{X2bGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXXKemVOPzJiaILz MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWRTD2xJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJI9zKEOFSz24JIF{e2G7LDDHTVUxKD1iMD6wNFEh|ryPLh?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV2NEG0PUc,Ojl3NESxOFk9N2F-
GISTT1 NWDYcIg4SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NELMbZY4OiCqcoO= NFn2cVBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFfJV3RVOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhT0l3MDC9JFAvODB|IN88UU4> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV2MU[5OUc,Ojh3NEG2PVU9N2F-
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GISTT1 NXXifGNlSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYLmOmNVPzJiaILz MoDHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDjT2lVKGSncHXu[IVvfCCqdX3hckBIUVOWVEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYKt[4xwN0OFS{igZZN{[XluIFfJOVAhRSByLkCwPEDPxE1w M3u2cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
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GISTT1 M3fZTmZ2dmO2aX;uJIF{e2G7 NULje4NWPzJiaILz MXTJcohq[mm2aX;uJI9nKEuLVDDpckBpfW2jbjDHTXNVXDFiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiR1m1NEA:KDBwMEGg{txONg>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd5M{G1N{c,OjN5N{OxOVM9N2F-
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BA/F3 NFjuemRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkjIOFghcHK| MWDHdo94fGhiaX7obYJqfGmxbjDv[kBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKHerbHSteJlx\SCEY4KtRYJtKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjB6OTFOwG0v M1rW[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[yNlE4Lz5{NkW2NlIyPzxxYU6=
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Ba/F3 NWfH[IJQTnWwY4Tpc44h[XO|YYm= Ml;uOFghcHK| NFvURmFKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDCR3IuSUKOMTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC0PEBpenNiYomgRpJqfGWOaXfoeEBtfWOrZnXyZZNmKGG|c3H5MEBIUTVyIE2gNE4xQTB3IN88UU4> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF|N{m4NUc,OzBzM{e5PFE9N2F-
BA/F3 NYflNmN6S3m2b4TvfIlkcXS7IHHzd4F6 MVm0PEBpenN? MmLVR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMhfHKjboPm[YN1\WRid3n0bEB4cWymIIT5dIUhSmO{LVHicEBi\nSncjC0PEBpenNiYomgXHRVKGG|c3H5MEBKSzVyIE2gNE4xQTJizszNMi=> NEfXV2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFgxPid-MkO2NFA5ODZ:L3G+
GIST882 NVnNSppzTnWwY4Tpc44h[XO|YYm= MkjUTY5pcWKrdHnvckBw\iCqdX3hckBMUVRiYYX0c5Bpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDHTXNVQDh{IHPlcIx{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yOUeg{txONg>? NHfFVmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEixO|U{QCd-MkC4NVc2Ozh:L3G+
GIST882 Ml3lSpVv[3Srb36gZZN{[Xl? NF3qWlRKdmirYnn0bY9vKG:oIFvJWEBMPjR{RTDteZRidnRiYYX0c5Bpd3OyaH;yfYxifGmxbjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBpfW2jbjDHTXNVQDh{IHPlcIx{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yOUeg{txONg>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzMUe3NUc,OjN4MUG3O|E9N2F-
insect NXfSUIJWTnWwY4Tpc44h[XO|YYm= MW[zNEBucW6| NWXRVW1rUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDD3bYxlKHS7cHWgRWJNOSCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KGGodHXyJFMxKG2rboOgZpkhTlKHVDDhd5NigSxiSVO1NEA:KDBwMEm4NkDPxE1w NVH1SYdERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4ODNpPkKzN|AyPzB|PD;hQi=>
K562 NIO4T2xEgXSxdH;4bYNqfHliYYPzZZk> M37mblczKGi{cx?= MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDhcIFu[XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMTFOwG0v NWP4PGo{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmzNFE6ODJpPkG5N|AyQTB{PD;hQi=>
primary leukemia cells M1Tyd2N6fG:2b4jpZ4l1gSCjc4PhfS=> MojXO|IhcHK| NIr2T4JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBxemmvYYL5JIxmfWunbXnhJINmdGy|IHnzc4xifGWmIH\yc40h[WO3dHWgcZlmdG:rZDDs[ZVs\W2rYTDwZZRq\W62IHX4dJJme3Orbnege4lt\CC2eYDlJGZNXDNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYYPzZZktKEmFNUCgQUAxNjFizszNMi=> MljRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkGyNFEoRjJ{MkKxNlAyRC:jPh?=
BV173 M4fodGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MUS0PEBpenN? MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKYMUezJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsMXRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygS2k2OCB;IECuNUDPxE1w M4PrTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEGxNVU6Lz5{N{CxNVE2QTxxYU6=
BAF3 MkPnSpVv[3Srb36gZZN{[Xl? NGfNfnc4OiCqcoO= MofuTY5pcWKrdHnvckBw\iCWZXyt[pV{\WRiY1vJWEBNPTZ5UDDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRWY{KGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LXfsc{9ES0t6IHHzd4F6NCCJSUWwJF0hOC5zIN88UU4> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
K562 MVvDfZRwfG:6aXPpeJkh[XO|YYm= Mk\TNlQhcHK| MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlEh|ryPLh?= NV3yTlJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2N|I6OzVpPkKyOlMzQTN3PD;hQi=>
BA/F3 NXnlRmZNTnWwY4Tpc44h[XO|YYm= NVzpN5ZUPzJiaILz NH\sW3pKdmirYnn0bY9vKG:oIGTFUE1nfXOnZDDQSGdHWmKndHGgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMUCyJO69VS5? M1TZZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
BAF3 NWLLe4ZETnWwY4Tpc44h[XO|YYm= M1HCc|czKGi{cx?= MX7Jcohq[mm2aX;uJI9nKFSnbD3meZNm\CClLVvJWEBNPTd4UDDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gRmFHOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDvdkBES0t6IHHzd4F6NCCJSUWwJF0hOC5zMEKg{txONg>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl4Nkm1OEc,Ojd7Nk[5OVQ9N2F-
GIST882 NILPZnVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVvocIJISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDHTXNVQDh{IHPlcIx{NCCLQ{WwJF0hOC5zMEig{txONg>? M3;rZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEG3OVM5Lz5{MEixO|U{QDxxYU6=
GIST882 M4CxXGZ2dmO2aX;uJIF{e2G7 MXvJcohq[mm2aX;uJI9nKEuLVDDLOlQzTSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hT0mVVEi4NkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHL5JGFVWC2mZYDs[ZRqd25iYYPzZZktKEmFNUCgQUAxNjFyODFOwG0v NEXYNJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xNVc4OSd-MkO2NVE4PzF:L3G+
K562 Mo\jR5l1d3SxeHnjbZR6KGG|c3H5 MXfDfZRwfG:6aXOg[YZn\WO2IHnuJGs2PjJiY3XscJMtKEmFNUCgQUAxNjFzIN88UU4> MkHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJ7NUGxNVMoRjF{OUWxNVE{RC:jPh?=
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BA/F3 NE\4UlFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mn\aO|IhcHK| NXzXNFdvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEKlcj3BZowhUDN7NmCgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OCB;IECuNVEh|ryPLh?= M3\IVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEi4OlQ1Lz5{M{C4PFY1PDxxYU6=
BAF3 NVzSc|h2TnWwY4Tpc44h[XO|YYm= NF7POJA4OiCqcoO= NUi1OI9FUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgR3NHOVJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gRmFHOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDvdkBES0t6IHHzd4F6NCCJSUWwJF0hOC5zMTFOwG0v NHnDNmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m2Olk2PCd-Mke5OlY6PTR:L3G+
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insect cells MV3GeY5kfGmxbjDhd5NigQ>? NYTUTlJxOzBibXnudy=> MYrJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEGETEGgUVM2OVRibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMh[W[2ZYKgN|AhdWmwczDifUBHWkWWIHHzd4F6NCCLQ{WwJF0hOC5zMUSzJO69VS5? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNyMUewN{c,OjN|MEG3NFM9N2F-
insect cells NYHvemNkTnWwY4Tpc44h[XO|YYm= M1\DRlMxKG2rboO= NInQUnhKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFHCUFEhWTJ3MligcZV1[W62IHX4dJJme3OnZDDpckBqdnOnY4SgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIUlXUJIF{e2G7LDDJR|UxKD1iMD6xNVUh|ryPLh?= NFfhWJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwNVcxOyd-MkOzNFE4ODN:L3G+
K562 MkPaRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MVq3NkBpenN? MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLDVk1CSkxiZHXw[Y5l\W62IHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYKt[4xwN0OFS{igZZN{[XluIFfJOVAhRSByLkGyJO69VS5? MlTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
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Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-STAT5 / STAT5 ; p-ZAP70 / ZAP70 / p-LAT / LAT 18981115
Immunofluorescence RelB ; Cortactin / F-actin 20371728 20937825
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • Animal Models: SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
  • Dosages: 70 or 100 mg/kg
  • Administration: Administered via i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 118 mg/mL
(200.09 mM)
Water 118 mg/mL
(200.09 mM)
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 589.71
Formula

C29H31N7O.CH4SO3

CAS No. 220127-57-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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.CS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02687425 Unknown status Drug: Pioglitazone|Drug: imatinib mesylate Leukemia Myelogenous Chronic BCR-ABL Positive Meng Li|Tongji Hospital February 2016 Phase 2
NCT02303899 Completed Drug: Gemcitabine|Drug: Imatinib mesylate Mesothelioma Malignant Istituto Clinico Humanitas November 2014 Phase 2
NCT01898377 Terminated Drug: Imatinib mesylate Mycophenolate mofetil Chronic Graft-versus-host Disease Seoul National University Hospital August 2013 Phase 2
NCT02891395 Completed Drug: Imatinib Mesylate and Nilotinib Graft Versus Host Disease University Hospital Lille|Novartis December 24 2012 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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

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