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 212 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
GIST882 M{fJcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:5OkBp NU[1XopSUUN3ME2xMlch|ryP NFrxdZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFIyOid-MkS5NFAzOTJ:L3G+
K562 NV;CdYpMS3m2b4TvfIlkcXS7IFHzd4F6 Mo\JNlQhcA>? NFT1enNKSzVyPUCuNlEh|ryP MkP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyMECyNFcoRjJ{MECwNlA4RC:jPh?=
MCF-7 MYHDfZRwfG:6aXPpeJkhSXO|YYm= MXmyOEBp MX3JR|UxRTBwOEOg{txO NGnpVpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkCwNFIxPyd-MkKwNFAzODd:L3G+
MDA-MB-23 MX;DfZRwfG:6aXPpeJkhSXO|YYm= MUOyOEBp MnmxTWM2OD1zLkig{txO NFfaNoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkCwNFIxPyd-MkKwNFAzODd:L3G+
K562r Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvudVVrUUN3ME2xNOKh|ryP NXvneYFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5N|k1OThpPkK0PVM6PDF6PD;hQi=>
K562 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTFR|UxRTBwMEmg{txO Mn\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ4N{i0NVQoRjF4Nke4OFE1RC:jPh?=
MCF-7 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j6S|ExKM7:TR?= NHe4WmI1QCCq MmDxZoxw[2u|IHPlcIwheHKxbHnm[ZJifGmxbjDpcoNz\WG|ZTDpcoR2[2WmIHL5JGJLO1p? Ml7LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{SwN|QoRjJ3Mke0NFM1RC:jPh?=
K-562  NIHwbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXhbY1[UUN3ME2xJO69VQ>? MkiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{M{m2OlIoRjJ3MkO5OlYzRC:jPh?=
K562  NGTQfItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Tp[2lEPTB;MD61xsDPxE1? NF;Lb2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmzPVQyQCd-MkS5N|k1OTh:L3G+
PC3  NFKyc5dCeG:ydH;zbZMhSXO|YYm= M{fpZ|Ix6oDLzszN NVXQXGVTPDhxN{KgbC=> M{jmXYlv[3KnYYPld{Bk\WyuIIP1dpZqfmGu MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd6Nk[1Okc,OjV5OE[2OVY9N2F-
PC3  NU\aOow6S2WubDDWbYFjcWyrdImgRZN{[Xl? MVWyNQKBkc7:TR?= MmHzOk04OiCq NELIclNqdmO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= M3O2TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{i2OlU3Lz5{NUe4OlY2PjxxYU6=
DU145 Mlm4RZBweHSxc3nzJGF{e2G7 NIHIO4YzOOLCid88US=> NETaeYc1QC95MjDo M4HSRolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCjcH;weI9{cXN? NI\MbVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe4OlY2Pid-MkW3PFY3PTZ:L3G+
DU145 MnTQR4VtdCCYaXHibYxqfHliQYPzZZk> MU[yNQKBkc7:TR?= NEG1cos3NTd{IHi= NGnkS3Rl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NI\Zelc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe4OlY2Pid-MkW3PFY3PTZ:L3G+
Hep G2 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fubWlEPTB;M{Gg{txO M2rsfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[zNlMzLz5{NUi2N|I{OjxxYU6=
T47D  NVzJbnRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTlVGp4UUN3ME21NEDPxE1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4M{KzNkc,OjV6NkOyN|I9N2F-
EOL-1 MlW0R5l1d3SxeHnjbZR6KGG|c3H5 MXu3NkBpenN? MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDFU2wuOSClZXzsd{Bi\nSncjC3NkBpenNiYomgZYxidWG{LXLseYUh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkCwNFIh|ryPLh?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTNyMUmwNkc,OTl|MEG5NFI9N2F-
EOL-1 MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{jrUFczKGi{cx?= MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWRTD2xJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJI9zKEOFSz24JIF{e2G7LDDHTVUxKD1iMD6wNFEh|ryPLh?= NFG1TG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0OFE1QSd-Mkm1OFQyPDl:L3G+
GISTT1 NFTEOWJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEnDeYI4OiCqcoO= MnzORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCJSWPUWFEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGdKPTBiPTCwMlAxOyEQvF2u MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV2MU[5OUc,Ojh3NEG2PVU9N2F-
Sf9 M4rYfmZ2dmO2aX;uJIF{e2G7 NFXCNoVDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFkfGm4ZTDzbZRmKG:oIF6teIVzdWmwYXygbIV5[Wirc4Tp[Ilv\S22YXfn[YQhSUKOMjDlfJBz\XO|ZXSgbY4hXHKrY3jvdIx2e2mjIH7pJIlv\mWldHXkJHNnQSClZXzsd{BjgSCrc3;0bIVzdWGuIITpeJJifGmxbjDjZYxwemmvZYTybYMh[XO|YYmsJGtlKD1iMD6wNFYh|ryPLh?= M{DVPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEG3N|Q{Lz5{MUSxO|M1OzxxYU6=
K562 NYXWTXZQSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MoTBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCrbXH0bY5q[i2{ZYPpd5RidnRiS{W2NkBk\WyuczygTWM2OCB;IECuNFA3ODVizszNMi=> Mn[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{[1PFcoRjJzM{e2OVg4RC:jPh?=
GISTT1 Mm\CRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MVi3NkBpenN? NE\adZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JINMUVRiZHXw[Y5l\W62IHj1cYFvKEeLU2TUNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IECuNFA5KM7:TT6= MlvUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
GISTT1 MonDRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NF3mXnU4OiCqcoO= MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEeLU2TUNUBk\WyuczDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BweiCFQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNFgh|ryPLh?= MoSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7Nk[5OVQoRjJ5OU[2PVU1RC:jPh?=
GISTT1 M3r2WGZ2dmO2aX;uJIF{e2G7 MVO3NkBpenN? NHTFN3pKdmirYnn0bY9vKG:oIFvJWEBqdiCqdX3hckBIUVOWVEGgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygS2k2OCB;IECuNFEh|ryPLh?= M1jhbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{ezNVU{Lz5{M{e3N|E2OzxxYU6=
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GIST882 M{HoPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M2e1bVczKGi{cx?= MlXORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDjT2lVKGSncHXu[IVvfCCqdX3hckBIUVOWOEiyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNVQh|ryPLh?= MneyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
GIST882 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NX;QNIlSPzJiaILz M{jXU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iR1nTWFg5OiClZXzsd{Bu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCxcjDDR2s5KGG|c3H5MEBIUTVyIE2gNE4xOTRizszNMi=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl4Nkm1OEc,Ojd7Nk[5OVQ9N2F-
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GIST882 MmrCRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{K1O|czKGi{cx?= M4\LZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iR1nTWFg5OiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhT0l3MDC9JFAvODJizszNMi=> MmDQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3NEG2PVUoRjJ6NUSxOlk2RC:jPh?=
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BA/F3 MoDJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFyweYQ1QCCqcoO= NIPFWopIem:5dHigbY5pcWKrdHnvckBw\iCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIIfpcIQufHmyZTDCZ5IuSWKuIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkC4PUDPxE1w NF7sbpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2NlIyPyd-Mk[1OlIzOTd:L3G+
K562 NXvxdnp4TnWwY4Tpc44h[XO|YYm= NX;zbY9VOzBibXnudy=> MVrJcohq[mm2aX;uJI9nKGurbn;i[YFlKGKrbnTpcochfG9iRFTSNUBqdiCqdX3hckBMPTZ{IHPlcIx{KGmwY4XiZZRm\CCob4KgN|AhdWmwczDifUBqXFKDUTDy[YFo\W62LXLhd4VlKG2jc4Ogd5Bm[3S{b33leJJq[yCvZYToc4QtKEmFNUCgQUAxNjB7IN88UU4> MknRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
Ba/F3 NUTNWIcxTnWwY4Tpc44h[XO|YYm= M2XYdFQ5KGi{cx?= NHruZZpKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDCR3IuSUKOMTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC0PEBpenNiYomgRpJqfGWOaXfoeEBtfWOrZnXyZZNmKGG|c3H5MEBIUTVyIE2gNE4xQTB3IN88UU4> MoP2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzM{e5PFEoRjNyMUO3PVgyRC:jPh?=
BA/F3 NEe2NnJEgXSxdH;4bYNqfHliYYPzZZk> Ml\nOFghcHK| M3f5W2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z|IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghf2muZDD0fZBmKEKlcj3BZowh[W[2ZYKgOFghcHK|IHL5JHhVXCCjc4PhfUwhUUN3MDC9JFAvODl{IN88UU4> NGPUVXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNFgxPid-MkO2NFA5ODZ:L3G+
GIST882 NITMNFdHfW6ldHnvckBie3OjeR?= M2rhVWlvcGmkaYTpc44hd2ZiaIXtZY4hU0mWIHH1eI9xcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gS2lUXDh6MjDj[YxteyCkeTDFUGlUSSxiSVO1NEA:KDBwMEm3JO69VS5? NVTzR5F7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4NVc2OzhpPkKwPFE4PTN6PD;hQi=>
GIST882 MYDGeY5kfGmxbjDhd5NigQ>? M3jGOmlvcGmkaYTpc44hd2ZiS1nUJGs3PDKHIH31eIFvfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIFfJV3Q5QDJiY3XscJMh[nliRVzJV2EtKEmFNUCgQUAxNjB7NzFOwG0v M1LDVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkGxO|cyLz5{M{[xNVc4OTxxYU6=
insect MXPGeY5kfGmxbjDhd5NigQ>? MWSzNEBucW6| MUnJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KHerbHSgeJlx\SCDQlyxJIV5eHKnc4Pl[EBqdiCrboPlZ5Qh[2WubIOgZYZ1\XJiM{CgcYlveyCkeTDGVmVVKGG|c3H5MEBKSzVyIE2gNE4xQTh{IN88UU4> M1Hid|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CxO|A{Lz5{M{OwNVcxOzxxYU6=
K562 NGPaNHZEgXSxdH;4bYNqfHliYYPzZZk> NX3GVZhSPzJiaILz NX\hbGtjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA4OiCqcoOgZpkh[WyjbXHyMYJtfWViY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlEh|ryPLh?= MnzyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|MEG5NFIoRjF7M{CxPVAzRC:jPh?=
primary leukemia cells M{DJV2N6fG:2b4jpZ4l1gSCjc4PhfS=> M1HsPVczKGi{cx?= NV\HUFN6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4heHKrbXHyfUBt\XWtZX3pZUBk\WyuczDpd49t[XSnZDDmdo9uKGGldYTlJI16\WyxaXSgcIV2c2WvaXGgdIF1cWWwdDDlfJBz\XO|aX7nJJdqdGRidInw[UBHVFR|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHHzd4F6NCCLQ{WwJF0hOC5zIN88UU4> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{MUKwNUc,OjJ{MkGyNFE9N2F-
BV173 NUDj[Fg4SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFfaN4Q1QCCqcoO= MljCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVkG3N{Bk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscE1VcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGdKPTBiPTCwMlEh|ryPLh?= MmG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMUGxOVkoRjJ5MEGxNVU6RC:jPh?=
BAF3 NFfDU5dHfW6ldHnvckBie3OjeR?= NVnpN5dqPzJiaILz MVnJcohq[mm2aX;uJI9nKFSnbD3meZNm\CClS1nUJGw2PjeSIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBSlMh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSClZXzseIl1\XJvZ3zvM2NEUzhiYYPzZZktKEeLNUCgQUAxNjFizszNMi=> NFW3NlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
K562 NVWxbHZwS3m2b4TvfIlkcXS7IHHzd4F6 NYPEW2lKOjRiaILz NHPlNmpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjFizszNMi=> NHLSWmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[zNlk{PSd-MkK2N|I6OzV:L3G+
BA/F3 MYHGeY5kfGmxbjDhd5NigQ>? M1;6dVczKGi{cx?= MnjvTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUFTHSnJj\XSjIDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjFyMjFOwG0v MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BAF3 NGezSXNHfW6ldHnvckBie3OjeR?= MVy3NkBpenN? NYTQUIhJUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgZ{1MUVRiTEW3OnAhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEKDRkOgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hd3JiQ1PLPEBie3OjeTygS2k2OCB;IECuNVAzKM7:TT6= NH;5fHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m2Olk2PCd-Mke5OlY6PTR:L3G+
GIST882 NWTQXmtWSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NIfYbI5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFfJV3Q5QDJiY3XscJMtKEmFNUCgQUAxNjFyODFOwG0v MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODhzN{WzPEc,OjB6MUe1N|g9N2F-
GIST882 NVX2UGFYTnWwY4Tpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKEuLVDDLOlQzTSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hT0mVVEi4NkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHL5JGFVWC2mZYDs[ZRqd25iYYPzZZktKEmFNUCgQUAxNjFyODFOwG0v MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzMUe3NUc,OjN4MUG3O|E9N2F-
K562 MYLDfZRwfG:6aXPpeJkh[XO|YYm= M4\4NWN6fG:2b4jpZ{Bm\m[nY4SgbY4hUzV4MjDj[YxteyxiSVO1NEA:KDBwMUGg{txONg>? NFLCeWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkm1NVEyOyd-MUK5OVEyOTN:L3G+
KU812 NYrsfGQ3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXy3NkBpenN? M3H0fWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS2W4NVIh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGdKPTBiPTCwMlEyKM7:TT6= M2TPXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUSxOlk2Lz5{OEW0NVY6PTxxYU6=
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BAF3 M4f6dGZ2dmO2aX;uJIF{e2G7 M4G0WlczKGi{cx?= NWHkSGlNUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgR3NHOVJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gRmFHOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDvdkBES0t6IHHzd4F6NCCJSUWwJF0hOC5zMTFOwG0v MoDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7Nk[5OVQoRjJ5OU[2PVU1RC:jPh?=
32D Ml7TRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NEnlSlg1QCCqcoO= MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKDN{RDDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKHB{MUCgZ4VtdHNiZYjwdoV{e2mwZzDCZ5Iu[WKuIHHzd4V{e2WmIHHzJJBzd2yrZnXyZZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMUGyJO69VS5? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjRzNUi2N{c,OTZ2MUW4OlM9N2F-
insect cells NFrlV4lHfW6ldHnvckBie3OjeR?= M1zjPFMxKG2rboO= NXHL[2dmUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDBRmwyKE1|NUHUJI12fGGwdDDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRmLFWEBie3OjeTygTWM2OCB;IECuNVE1OyEQvF2u NXnoV3ozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4ODNpPkKzN|AyPzB|PD;hQi=>
insect cells MoG1SpVv[3Srb36gZZN{[Xl? MYezNEBucW6| MWTJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEGETEGgVVI2OkhibYX0ZY51KGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMh[W[2ZYKgN|AhdWmwczDifUBHWkWWIHHzd4F6NCCLQ{WwJF0hOC5zMUWg{txONg>? NXS3dYp2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFE4ODNpPkKzN|AyPzB|PD;hQi=>
K562 NI[5VpJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M330T|czKGi{cx?= M1fGfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRmNTNUGETDDk[ZBmdmSnboSgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IECuNVIh|ryPLh?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
BA/F3 MoW3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MkDoO|IhcHK| NWrDcHB7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEKlcj3BZowhVTJ2NG[gcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OCB;IECuNVI6KM7:TT6= M3[3WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEi4OlQ1Lz5{M{C4PFY1PDxxYU6=
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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.
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.

Solubility (25°C)

In vitro

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)

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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.

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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 2022-01-17)

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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