Imatinib (STI571)

For research use only. Not for use in humans.

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 746.33 现货
RMB 571.38 现货
RMB 980.11 现货
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客户使用Selleck生产的Imatinib (STI571)发表文献134篇:

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 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzld29JUUN3ME2wMlA4OzB2IN88US=> NVXx[XdOW0GQR1XS
EM-2 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3WzZWlEPTB;MD6wPFg5KM7:TR?= M{HlNnNCVkeHUh?=
MEG-01 NEDpcHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TwcWlEPTB;MD6wPFkzOSEQvF2= M4TpUnNCVkeHUh?=
BV-173 M3vodWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzMZnRKSzVyPUCuNVg4PCEQvF2= MUDTRW5ITVJ?
K-562 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NECwdFFKSzVyPUCuNlI1OzJizszN NYqycY1[W0GQR1XS
CGTH-W-1 NYL1eJRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK2T4xLUUN3ME2wMlM5Ozd2IN88US=> M1LjSnNCVkeHUh?=
ST486 MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XVe2lEPTB;MD62PFU1KM7:TR?= NWPm[4R7W0GQR1XS
NCI-H1436 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvwTWM2OD1yLkm3PFAyKM7:TR?= M2LzW3NCVkeHUh?=
NOS-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFwNkWzPFMh|ryP MlPNV2FPT0WU
A498 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLBO2hKSzVyPUKuOVczOjNizszN MkjvV2FPT0WU
BE-13 MoO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;sflkyUUN3ME2yMlYzOTB4IN88US=> NXPkWFdoW0GQR1XS
SUP-T1 M3\VeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfSXXdKSzVyPUOuPFI6ODdizszN MnzLV2FPT0WU
NCI-H1770 M4H6UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTVwNUeyOlIh|ryP NWnEb4lJW0GQR1XS
IMR-5 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7WTWM2OD14LkKyNVQ4KM7:TR?= NX:wR2ZpW0GQR1XS
LB2241-RCC M{DNe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHzUIpKSzVyPUiuNFc{QDRizszN NEDOUIZUSU6JRWK=
TGBC24TKB M4L5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRThwM{SwOVIh|ryP NHL3TIRUSU6JRWK=
SCC-15 M33xOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLRTWM2OD1zMD63O|g5KM7:TR?= M1K2eHNCVkeHUh?=
BB49-HNC NUTrfZFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPiTWM2OD1zND6zN|M2KM7:TR?= NIrCU|BUSU6JRWK=
ES7 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36yb2lEPTB;MUSuO|M4QSEQvF2= NWjTZ5hDW0GQR1XS
LB2518-MEL NFe0RWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTF4Lk[wPVQh|ryP MVLTRW5ITVJ?
NCI-H510A M3K3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3PTWM2OD1zNz6yOFQzKM7:TR?= Mnv5V2FPT0WU
TE-441-T MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTF5LkK4PFYh|ryP MoWxV2FPT0WU
HH NGT6TW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHWRnZKSzVyPUG3MlM6QTlizszN NG\2VlFUSU6JRWK=
LC4-1 M2THdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3EeIFKSzVyPUG4MlA3PTJizszN M3XmRXNCVkeHUh?=
KARPAS-45 Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke3TWM2OD1zOD6xPFQ5KM7:TR?= NVvMNFBDW0GQR1XS
LB1047-RCC M2f5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf2TWM2OD1zOD60OFUzKM7:TR?= MlnxV2FPT0WU
NKM-1 NYraTI1HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPlOo5sUUN3ME2xPU4{PTV{IN88US=> MU\TRW5ITVJ?
SCLC-21H MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzON4lKSzVyPUKwMlEzPDZizszN M3jmcHNCVkeHUh?=
RS4-11 NILLWIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;4OGlEPTB;MkCuN|MxQCEQvF2= NETydHJUSU6JRWK=
ALL-PO M37kbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHKeG5KSzVyPUKwMlgyPDlizszN MVnTRW5ITVJ?
GDM-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVGyemozUUN3ME2yNk42QTR3IN88US=> NYjIfmJlW0GQR1XS
DMS-79 NWPCR3B4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvNTWM2OD1{ND60PVM1KM7:TR?= MnvuV2FPT0WU
MPP-89 MomxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzuTIg4UUN3ME2yOU43QDd2IN88US=> MUDTRW5ITVJ?
NB10 M{TLNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvCZ3JKSzVyPUK2MlQ3QTlizszN NWDMXI9[W0GQR1XS
LS-513 NHLCSXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjLNFk4UUN3ME2yOk45QDR5IN88US=> NWDORZI5W0GQR1XS
L-540 NGfNSWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjmRZlIUUN3ME2yOk46OTR|IN88US=> MlPZV2FPT0WU
ES1 M2XzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzPTWM2OD1{Nz61NlEh|ryP NIn0dlFUSU6JRWK=
NTERA-S-cl-D1 MkfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTNyLkWwPVMh|ryP NV7RN2JZW0GQR1XS
EW-1 MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWeyW3B5UUN3ME2zNk46PDV2IN88US=> M1nofXNCVkeHUh?=
Calu-6 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLJTWM2OD1|Mz6xPFU2KM7:TR?= MWnTRW5ITVJ?
CTV-1 Mo\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXVSWNLUUN3ME2zN{46Pzh7IN88US=> Mm[xV2FPT0WU
YT MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm2OopKSzVyPUO4MlUzODlizszN MWTTRW5ITVJ?
TE-6 MnPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDwXYIxUUN3ME20NU4zPzl6IN88US=> NH3EUlFUSU6JRWK=
HT-144 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nhSWlEPTB;NEGuOVQ5PiEQvF2= MlnpV2FPT0WU
EW-13 NXLNeoVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jl[GlEPTB;NEKuNlc6OSEQvF2= NIW0eGFUSU6JRWK=
KALS-1 MkfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zDVGlEPTB;NEOuNVMzQSEQvF2= M2fP[nNCVkeHUh?=
MOLT-16 NEXVSZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4mzRWlEPTB;NEWuNFc2OiEQvF2= MlPnV2FPT0WU
D-336MG MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi0WlRjUUN3ME20OU46PTl7IN88US=> NI\iPZpUSU6JRWK=
TE-11 M3rkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHIdGFlUUN3ME20Ok43PTNizszN M{DXN3NCVkeHUh?=
EB2 MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;yWVlKSzVyPUS2MlY6QSEQvF2= MXrTRW5ITVJ?
SK-N-DZ MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjsOFdKSzVyPUS4MlA6PjFizszN MXrTRW5ITVJ?
SW684 MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XtdWlEPTB;NEiuNlY6PSEQvF2= M1\FbXNCVkeHUh?=
EW-18 M1r0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHQeZFKSzVyPUS4MlQ{QTVizszN MVzTRW5ITVJ?
RL95-2 MkDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTVyLkC3NUDPxE1? NGX6XVlUSU6JRWK=
CHP-126 M2nzeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jNOGlEPTB;NUCuPFkxPSEQvF2= NGL1[JdUSU6JRWK=
NCI-H1395 NI\ZdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\tTWM2OD13MT63PFM2KM7:TR?= MkP6V2FPT0WU
TE-15 M3\GOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHvTWM2OD13Mj6yOVU3KM7:TR?= M4jVb3NCVkeHUh?=
ES4 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vZbmlEPTB;NUKuPVc4PSEQvF2= NE\Q[o9USU6JRWK=
TE-1 NIPL[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnYbY9KSzVyPUWzMlk1PTVizszN NEjIVHFUSU6JRWK=
SIMA NFfo[ZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTV5LkOzNVEh|ryP M1XqUXNCVkeHUh?=
LB647-SCLC Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LBWWlEPTB;NkSuNVE5QCEQvF2= M3nTNXNCVkeHUh?=
KY821 NEDid3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvxTWM2OD14ND6yOVUzKM7:TR?= NEfqNFNUSU6JRWK=
LC-2-ad NGHtd3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL5TWM2OD14NT63OlAyKM7:TR?= NUfOfpNzW0GQR1XS
KP-N-RT-BM-1 NETZT2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\uR2lEPTB;Nk[uOlM3PiEQvF2= NF;6WHFUSU6JRWK=
SW872 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTZ5LkSzPFIh|ryP MXvTRW5ITVJ?
ES5 M1L5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[3V5VKSzVyPU[3MlY6PjhizszN MX;TRW5ITVJ?
SK-NEP-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTZ6LkO4NFMh|ryP Ml3tV2FPT0WU
RPMI-6666 MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rmSmlEPTB;N{GuNFMzKM7:TR?= MYTTRW5ITVJ?
UACC-812 NWn3S3VVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVno[FYxUUN3ME23NU4yPjB7IN88US=> M4D4c3NCVkeHUh?=
COLO-829 NVXSfYtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTd{Lk[5PFch|ryP MonwV2FPT0WU
KP-N-YS NUTa[YtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrqZY9KSzVyPUeyMlcyOzlizszN MkTNV2FPT0WU
GI-1 NUPJ[|hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DCWWlEPTB;N{OuNlg3QCEQvF2= M13DXnNCVkeHUh?=
ETK-1 NEHZPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHWTWM2OD15Mz60PVMzKM7:TR?= MWfTRW5ITVJ?
LXF-289 M2jBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\kTWM2OD15Mz63Nlkh|ryP NXOzVGE4W0GQR1XS
CAS-1 M3q0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX75SG5GUUN3ME23N{45QDV5IN88US=> M2ThfHNCVkeHUh?=
EW-22 NXGwWZR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSxd|JKSzVyPUe0MlcyOTVizszN NV3QfG5kW0GQR1XS
NCI-H2196 NGTQWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe3dFU3UUN3ME23OU43Ozd7IN88US=> M{\LVXNCVkeHUh?=
EoL-1-cell NVHCc2F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHewOZBKSzVyPUixMlY6PjNizszN M4P2eHNCVkeHUh?=
D-247MG M4L5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoiwTWM2OD16Mj6wNlQ5KM7:TR?= M3i3XXNCVkeHUh?=
Becker M4CwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrvNGVKSzVyPUiyMlM1QDFizszN MnvsV2FPT0WU
IST-MEL1 NIq5Xo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluxTWM2OD16Mj6zOFgzKM7:TR?= NGXRSXVUSU6JRWK=
MDA-MB-134-VI M{Phc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDtdoFEUUN3ME24Nk42QTl4IN88US=> MVvTRW5ITVJ?
NCI-H1092 NWHheWdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jWSWlEPTB;OESuNFE6PyEQvF2= M{nSbXNCVkeHUh?=
KINGS-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X2NGlEPTB;OE[uNVYyQCEQvF2= MUnTRW5ITVJ?
HCC2218 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHtO21KSzVyPUi2Mlc6OTNizszN NX3RSFd6W0GQR1XS
GI-ME-N M2PHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnDTWM2OD16Nz63Olk6KM7:TR?= MVfTRW5ITVJ?
AM-38 MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;1VJI6UUN3ME24PE4{QTV|IN88US=> NXXoTI8xW0GQR1XS
KNS-42 NXnZNYRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTh7LkGwNVgh|ryP NGDLTVdUSU6JRWK=
C8166 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37EW2lEPTB;OEmuOlEzPSEQvF2= NULhZoJWW0GQR1XS
Ramos-2G6-4C10 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrCXIVRUUN3ME24PU45PzF7IN88US=> MmHlV2FPT0WU
CTB-1 NGTNZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fxV2lEPTB;OUCuOlM2PyEQvF2= MVnTRW5ITVJ?
HCE-4 MnnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrl[YlbUUN3ME25NU4yOzN4IN88US=> MW\TRW5ITVJ?
NCI-H526 NVn6[Wk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrVTWM2OD17Mj60NVA{KM7:TR?= M13aOHNCVkeHUh?=
ECC4 NFvi[IlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvOWJlkUUN3ME25OE4zPTV3IN88US=> MWDTRW5ITVJ?
NCCIT NHPYfm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzvfVBOUUN3ME25OU4{Ojl{IN88US=> MnjXV2FPT0WU
MZ7-mel M4nK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXoN3R{UUN3ME25OU46ODRizszN MWfTRW5ITVJ?
COLO-684 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XLdWlEPTB;OU[uNlM5PSEQvF2= MkfMV2FPT0WU
SU-DHL-1 M3LEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInOWohKSzVyPUm2Mlk5PDJizszN MmLiV2FPT0WU
SF126 NF\QNlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTl5LkWyNVch|ryP NX3rVHcyW0GQR1XS
NMC-G1 MnnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTl6LkS1OVQh|ryP NIHwU5lUSU6JRWK=
NB14 M3zSc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3juNmlEPTB;OUiuPVIxQCEQvF2= MonIV2FPT0WU
VA-ES-BJ M2XGNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHpTWM2OD17OT60NFU3KM7:TR?= NFnENpJUSU6JRWK=

... 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]

- 合并

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]

- 合并
  • 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)

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

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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
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

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