Imatinib (STI571)

目录号:S2475 别名: CGP057148B, ST-1571

Imatinib (STI571) Chemical Structure

Molecular Weight(MW): 493.6

Imatinib (STI571)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。

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产品安全说明书

PDGFR抑制剂选择性比较

生物活性

产品描述 Imatinib (STI571)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。
特性 Imatinib 是多靶点酪氨酸激酶抑制剂。
靶点
PDGFR [1]
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
体外研究

体外抑制一组酪氨酸和丝/苏氨酸蛋白激酶实验,说明Imatinib有效抑制v-Abl 酪氨酸激酶和PDGFR,IC50 分别为 0.6 和 0.1 μM。[1]Imatinib抑制 野生型 c-kit激酶活性的SLF依赖性激活,IC50约为0.1 μM, 与抑制PDGFR所需的浓度相似。[2] Imatinib 抑制人类支气管类癌细胞NCI-H727和胰腺类癌细胞 BON-1生长,IC50分别为 32.4 和 32.8 μM。[3] 最新研究显示Imatinib作用于慢性粒细胞白血病,通过下调hERG1 K(+)通道,具有恢复其抗白血病效果的潜力,而hERG1 K(+) 通道在白血病细胞中高表达,且易引发白血病。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LAMA-84 NVvEc|d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwMEezNFQh|ryP NFqwUIdUSU6JRWK=
EM-2 M2nhemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zK[2lEPTB;MD6wPFg5KM7:TR?= NHjCS3BUSU6JRWK=
MEG-01 NV3Cc3hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW5V|VKSzVyPUCuNFg6OjFizszN NVTFdoFpW0GQR1XS
BV-173 NYf1UGI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH22NXNKSzVyPUCuNVg4PCEQvF2= NI\Scm9USU6JRWK=
K-562 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTGTWM2OD1yLkKyOFMzKM7:TR?= NWq0W|A{W0GQR1XS
CGTH-W-1 MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGwfpVKSzVyPUCuN|g{PzRizszN M1fFfnNCVkeHUh?=
ST486 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG1R3FSUUN3ME2wMlY5PTRizszN MV3TRW5ITVJ?
NCI-H1436 NHjQc3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\YbmlEPTB;MD65O|gxOSEQvF2= NFH0[5dUSU6JRWK=
NOS-1 NUfnXVVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rzUGlEPTB;MT62OVM5OyEQvF2= NGXXeI9USU6JRWK=
A498 MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTJwNUeyNlMh|ryP NX64XZMxW0GQR1XS
BE-13 NFTVTVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTZOHNZUUN3ME2yMlYzOTB4IN88US=> MofNV2FPT0WU
SUP-T1 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2n0ZWlEPTB;Mz64NlkxPyEQvF2= MUXTRW5ITVJ?
NCI-H1770 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYftb2VkUUN3ME21MlU4OjZ{IN88US=> M{LQR3NCVkeHUh?=
IMR-5 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjBVnI6UUN3ME22MlIzOTR5IN88US=> MmLHV2FPT0WU
LB2241-RCC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LTeWlEPTB;OD6wO|M5PCEQvF2= NEDDb5pUSU6JRWK=
TGBC24TKB M1jic2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXi5cXQxUUN3ME24MlM1ODV{IN88US=> MmHwV2FPT0WU
SCC-15 M2jLfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\ic4RKSzVyPUGwMlc4QDhizszN MnftV2FPT0WU
BB49-HNC MlT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHHe4RKSzVyPUG0MlM{OzVizszN MUPTRW5ITVJ?
ES7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXKUHZvUUN3ME2xOE44Ozd7IN88US=> MmfEV2FPT0WU
LB2518-MEL M1XwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7sTWM2OD1zNj62NFk1KM7:TR?= MVfTRW5ITVJ?
NCI-H510A MoW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3m2SGlEPTB;MUeuNlQ1OiEQvF2= MmDXV2FPT0WU
TE-441-T NEC1UGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTF5LkK4PFYh|ryP MX7TRW5ITVJ?
HH MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfOTWM2OD1zNz6zPVk6KM7:TR?= MmnWV2FPT0WU
LC4-1 NFLoepdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nHfWlEPTB;MUiuNFY2OiEQvF2= NImwem9USU6JRWK=
KARPAS-45 MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrxTWM2OD1zOD6xPFQ5KM7:TR?= MmXuV2FPT0WU
LB1047-RCC M17ENGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofaTWM2OD1zOD60OFUzKM7:TR?= MUHTRW5ITVJ?
NKM-1 NXK3blA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\CR2lEPTB;MUmuN|U2OiEQvF2= NI\LU|VUSU6JRWK=
SCLC-21H NIqySo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\PVmlEPTB;MkCuNVI1PiEQvF2= NI[2bYVUSU6JRWK=
RS4-11 M3nBVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;sT2lEPTB;MkCuN|MxQCEQvF2= M4PnXXNCVkeHUh?=
ALL-PO NV\xfoZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnmTWM2OD1{MD64NVQ6KM7:TR?= MoTnV2FPT0WU
GDM-1 M3HBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LG[mlEPTB;MkKuOVk1PSEQvF2= NF:0NlBUSU6JRWK=
DMS-79 M{nPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\4SYxOUUN3ME2yOE41QTN2IN88US=> MmjJV2FPT0WU
MPP-89 M3fFO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33zOWlEPTB;MkWuOlg4PCEQvF2= MULTRW5ITVJ?
NB10 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTJ4LkS2PVkh|ryP Mn7hV2FPT0WU
LS-513 MnzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu2TWM2OD1{Nj64PFQ4KM7:TR?= NUfIXYpLW0GQR1XS
L-540 M{KzeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3HTWM2OD1{Nj65NVQ{KM7:TR?= MlnrV2FPT0WU
ES1 MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XOOGlEPTB;MkeuOVIyKM7:TR?= MoqyV2FPT0WU
NTERA-S-cl-D1 NHLlb|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\yTWM2OD1|MD61NFk{KM7:TR?= NXjNVoU4W0GQR1XS
EW-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHaTWM2OD1|Mj65OFU1KM7:TR?= M4Ln[nNCVkeHUh?=
Calu-6 NYn1b3UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXWTWM2OD1|Mz6xPFU2KM7:TR?= NETwVplUSU6JRWK=
CTV-1 NYrPVpJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTN|Lkm3PFkh|ryP Ml3tV2FPT0WU
YT NF\CRWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7TUYxKSzVyPUO4MlUzODlizszN MXvTRW5ITVJ?
TE-6 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DkWWlEPTB;NEGuNlc6QCEQvF2= NIrmWYZUSU6JRWK=
HT-144 M1;VTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PJe2lEPTB;NEGuOVQ5PiEQvF2= NWXvSlZQW0GQR1XS
EW-13 NXe3VIdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjWTWM2OD12Mj6yO|kyKM7:TR?= NIDtVHRUSU6JRWK=
KALS-1 NVm3RWtDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H1ZmlEPTB;NEOuNVMzQSEQvF2= NIfRZ5pUSU6JRWK=
MOLT-16 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR3LkC3OVIh|ryP M2\tWHNCVkeHUh?=
D-336MG NG\kcWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[zTWM2OD12NT65OVk6KM7:TR?= MlrXV2FPT0WU
TE-11 M{n2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIryenJKSzVyPUS2MlY2OyEQvF2= NXHPPZAxW0GQR1XS
EB2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTR4Lk[5PUDPxE1? NWjPTFlyW0GQR1XS
SK-N-DZ MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPnTWM2OD12OD6wPVYyKM7:TR?= MnrEV2FPT0WU
SW684 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPjUllKSzVyPUS4MlI3QTVizszN MUjTRW5ITVJ?
EW-18 NXfzeph2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTR6LkSzPVUh|ryP MoLJV2FPT0WU
RL95-2 NITnPWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTVyLkC3NUDPxE1? Ml3qV2FPT0WU
CHP-126 MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TVcWlEPTB;NUCuPFkxPSEQvF2= M1PQSXNCVkeHUh?=
NCI-H1395 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXwRmVWUUN3ME21NU44QDN3IN88US=> NG\2XINUSU6JRWK=
TE-15 NHi2UYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkO3TWM2OD13Mj6yOVU3KM7:TR?= MlPYV2FPT0WU
ES4 MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTV{Lkm3O|Uh|ryP MnH5V2FPT0WU
TE-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nXPGlEPTB;NUOuPVQ2PSEQvF2= MYjTRW5ITVJ?
SIMA M3vHRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPXTWM2OD13Nz6zN|EyKM7:TR?= NYjzW3IzW0GQR1XS
LB647-SCLC NWf4dnplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4juZ2lEPTB;NkSuNVE5QCEQvF2= M{W4VXNCVkeHUh?=
KY821 NF\CRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf2UlFUUUN3ME22OE4zPTV{IN88US=> NXHrRphnW0GQR1XS
LC-2-ad MkW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn5N3FKSzVyPU[1Mlc3ODFizszN Ml7oV2FPT0WU
KP-N-RT-BM-1 NXjENmduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSxbJVrUUN3ME22Ok43OzZ4IN88US=> Mlr0V2FPT0WU
SW872 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTZ5LkSzPFIh|ryP M2HWbHNCVkeHUh?=
ES5 NIjaepRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkWwTWM2OD14Nz62PVY5KM7:TR?= NF[zN3VUSU6JRWK=
SK-NEP-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP0PYdQUUN3ME22PE4{QDB|IN88US=> NHXGcG9USU6JRWK=
RPMI-6666 Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIL2eFNKSzVyPUexMlA{OiEQvF2= NIjyeZpUSU6JRWK=
UACC-812 NHjne5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjJZ5E1UUN3ME23NU4yPjB7IN88US=> M3nvdnNCVkeHUh?=
COLO-829 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTd{Lk[5PFch|ryP NHjvd|hUSU6JRWK=
KP-N-YS MkLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTd{LkexN|kh|ryP NXPnXZVmW0GQR1XS
GI-1 NXHZ[JpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvCPIlKSzVyPUezMlI5PjhizszN MkPwV2FPT0WU
ETK-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvnNnNKSzVyPUezMlQ6OzJizszN NUTCfGtvW0GQR1XS
LXF-289 NVzBVpRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDlU29KSzVyPUezMlczQSEQvF2= M2rsW3NCVkeHUh?=
CAS-1 NHrpWmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfldmNSUUN3ME23N{45QDV5IN88US=> NXjiWZd[W0GQR1XS
EW-22 M3ewemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfrSIdKSzVyPUe0MlcyOTVizszN MUHTRW5ITVJ?
NCI-H2196 NHvPXYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfV[Go{UUN3ME23OU43Ozd7IN88US=> NHzPOohUSU6JRWK=
EoL-1-cell MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m3dmlEPTB;OEGuOlk3OyEQvF2= NInLTHZUSU6JRWK=
D-247MG NEm2RYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DJe2lEPTB;OEKuNFI1QCEQvF2= M1\X[nNCVkeHUh?=
Becker NIXifnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPVTWM2OD16Mj6zOFgyKM7:TR?= NXLD[49WW0GQR1XS
IST-MEL1 NGHmbplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPPNWtKSzVyPUiyMlM1QDJizszN NIfnboNUSU6JRWK=
MDA-MB-134-VI M2DXVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTh{LkW5PVYh|ryP MVzTRW5ITVJ?
NCI-H1092 NGrjeXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXm[IppUUN3ME24OE4xOTl5IN88US=> M3yzU3NCVkeHUh?=
KINGS-1 NGTHV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLuTZVKSzVyPUi2MlE3OThizszN M2jxN3NCVkeHUh?=
HCC2218 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fHbWlEPTB;OE[uO|kyOyEQvF2= NFns[WdUSU6JRWK=
GI-ME-N Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPwTWM2OD16Nz63Olk6KM7:TR?= MXfTRW5ITVJ?
AM-38 NV20cHJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXoZ5lKSzVyPUi4MlM6PTNizszN M3XubnNCVkeHUh?=
KNS-42 NYXQ[FN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL6c5VNUUN3ME24PU4yODF6IN88US=> MoTlV2FPT0WU
C8166 NYrndlhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\lTWM2OD16OT62NVI2KM7:TR?= MmXvV2FPT0WU
Ramos-2G6-4C10 NY\PcFl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Xpb2lEPTB;OEmuPFcyQSEQvF2= M4LXVnNCVkeHUh?=
CTB-1 M1G2[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPQVGhKSzVyPUmwMlY{PTdizszN M2S0TnNCVkeHUh?=
HCE-4 M364Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTlW4FKSzVyPUmxMlE{OzZizszN NEnmeopUSU6JRWK=
NCI-H526 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTl{LkSxNFMh|ryP MlXHV2FPT0WU
ECC4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v5N2lEPTB;OUSuNlU2PSEQvF2= MVzTRW5ITVJ?
NCCIT MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1frRmlEPTB;OUWuN|I6OiEQvF2= NHvCeFdUSU6JRWK=
MZ7-mel NXjBRZl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfuTVVKSzVyPUm1MlkxPCEQvF2= NVHVW|dnW0GQR1XS
COLO-684 M4TO[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPKeJppUUN3ME25Ok4zOzh3IN88US=> M4HkSnNCVkeHUh?=
SU-DHL-1 Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HERmlEPTB;OU[uPVg1OiEQvF2= M3\4XXNCVkeHUh?=
SF126 NFvGUGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XaPGlEPTB;OUeuOVIyPyEQvF2= NE\YZYtUSU6JRWK=
NMC-G1 NYPGVW02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTl6LkS1OVQh|ryP MXzTRW5ITVJ?
NB14 M2T0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\3d|BKSzVyPUm4MlkzODhizszN MnrXV2FPT0WU
VA-ES-BJ MmPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTl7LkSwOVYh|ryP NXrPT5pZW0GQR1XS

... 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
体内研究 Imatinib作用于三种从新鲜人类小细胞肺癌衍生的移植瘤,具有不同的抗肿瘤效果,抑制SCLC6, SCLC61和 SCLC108 肿瘤生长分别达80%, 40% 和78%,而对SCLC74 生长没有明显抑制效果。[5] Imatinib 处理高脂肪饲喂的ApoE(-/-)小鼠, 显著降低高脂肪诱导的脂质染色区,按10,20和 40 mg/kg剂量饲喂,与未经高脂肪饮食处理的对照组相比,脂质染色区分别降低 30%, 27% 和 35%,且抑制颈动脉脂质堆积。[6]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

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PDGF 受体激酶活性 :

从BALB/c 3T3 细胞抽提物中使用兔抗血清免疫沉淀PDGF受体,然后小鼠PDGF受体置于冰上2小时。使用蛋白A-琼脂糖磁珠,用于收集抗原-抗体复合体。使用TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100)冲洗免疫沉淀反应两次,,使用TNE (50 mM Tris, pH 7.5, 140 mM EDTA)冲洗一次,再使用激酶 buffer (20 mM Tris, pH 7.5,10 mM MgCl2)冲洗一次。在 4oC下使用PDGF(50 ng/mL)刺激10分钟,在反应混合物中加入不同浓度Imatinib。与10 μCi [7-33P]-ATP及l μM ATP 在4oC下温育10分钟,然后测定PDGF受体激酶活性。通过 SDS-PAGE 在7.5% 凝胶上分离免疫复合物。
细胞实验:

[3]

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  • Cell lines: BON-1 和 NCI-H727 细胞
  • Concentrations: 0 到 100 μM
  • Incubation Time: 48 小时
  • Method:

    BON-1 细胞和 NCI-H727 细胞按一式三份接种在平底96孔板上,分别在补充10%胎牛血清的 DMEM 或 RPMI 1640 完全培养基中粘附过夜,更换培养基为无血清培养基(阴性对照) 或含连续稀释Imatinib的无血清培养基。48小时后 (对照组细胞不汇合),通过MTT实验测定代谢活性细胞数,使用Packard Spectra 酶标仪在540 nm处测定吸光值。按如下公式计算抑制生长率: 抑制率=(1 − a / b) × 100%, a 和 b 分别为实验组和对照组的吸光值。


    (Only for Reference)
动物实验:

[5]

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  • Animal Models: SCLC6, SCLC61, SCLC 74 和SCLC108小细胞注射进 Swiss小鼠 (nu/nu,雌性)
  • Formulation: Imatinib 在水中稀释
  • Dosages: 70 或 100 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 33 mg/mL (66.85 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
2mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 493.6
化学式

C29H31N7O

CAS号 152459-95-5
储存条件 粉状
溶于溶剂
别名 CGP057148B, ST-1571

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04097093 Not yet recruiting Other: No intervention GIST European Organisation for Research and Treatment of Cancer - EORTC December 1 2019 --
NCT03997903 Not yet recruiting Drug: Imatinib Mesylate Sickle Cell Disease Indiana University|Purdue University|Children''s Hospital Medical Center Cincinnati September 2019 Early Phase 1
NCT03891901 Not yet recruiting Drug: Imatinib|Drug: Isoniazid|Drug: Rifabutin Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) September 2019 Phase 2
NCT02644525 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
NCT03578367 Recruiting Drug: Asciminib add-on|Drug: Imatinib|Drug: Nilotinib CML|Chronic Myelogenous Leukemia|Leukemia Myeloid Chronic|Hematologic Diseases Novartis Pharmaceuticals|Novartis November 22 2018 Phase 2
NCT03454503 Not yet recruiting Drug: Imatinib Philadelphia Chromosome-positive Chronic Myeloid Leukemia in Chronic Phase Hikma Pharmaceuticals LLC May 2018 --

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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?

  • 回答:

    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.

  • 问题 2:

    What is the difference between S2475 (Imatinib) and S1026 (Imatinib Mesylate)? Are they water soluble?

  • 回答:

    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.

PDGFR Signaling Pathway Map

PDGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID