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。Imatinib (STI571) 可诱导自噬。

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157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。Imatinib (STI571) 可诱导自噬。
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 NV3W[5FMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwMEezNFQh|ryP NXXn[VVpW0GQR1XS
EM-2 MmL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXNXnRFUUN3ME2wMlA5QDhizszN MlLnV2FPT0WU
MEG-01 NH[2WXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfjco9KSzVyPUCuNFg6OjFizszN NHrrS3JUSU6JRWK=
BV-173 M4TibGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLmUFNxUUN3ME2wMlE5PzRizszN M4nnSnNCVkeHUh?=
K-562 MmH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPNTWM2OD1yLkKyOFMzKM7:TR?= MWjTRW5ITVJ?
CGTH-W-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTkOo9KSzVyPUCuN|g{PzRizszN NEDOOodUSU6JRWK=
ST486 MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLr[YtKSzVyPUCuOlg2PCEQvF2= NFrZWVVUSU6JRWK=
NCI-H1436 NWDGSlZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPtTWM2OD1yLkm3PFAyKM7:TR?= NXHJVpZNW0GQR1XS
NOS-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M371U2lEPTB;MT62OVM5OyEQvF2= NW\PWo5mW0GQR1XS
A498 NGT3eZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJwNUeyNlMh|ryP Mk\jV2FPT0WU
BE-13 NV\4b2huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHiUmh5UUN3ME2yMlYzOTB4IN88US=> M3npeXNCVkeHUh?=
SUP-T1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnj6TWM2OD1|LkiyPVA4KM7:TR?= MmjDV2FPT0WU
NCI-H1770 M4KzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTVwNUeyOlIh|ryP MnTJV2FPT0WU
IMR-5 MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTMTWM2OD14LkKyNVQ4KM7:TR?= Mn7pV2FPT0WU
LB2241-RCC MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHiWlhZUUN3ME24MlA4Ozh2IN88US=> NHrwXYlUSU6JRWK=
TGBC24TKB MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWq5XHJGUUN3ME24MlM1ODV{IN88US=> M4\UbXNCVkeHUh?=
SCC-15 MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPQU45KUUN3ME2xNE44Pzh6IN88US=> NVjHZ2lQW0GQR1XS
BB49-HNC NIjVbVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DnVGlEPTB;MUSuN|M{PSEQvF2= M4m4WHNCVkeHUh?=
ES7 M2TB[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf0TWM2OD1zND63N|c6KM7:TR?= NH7Bd5FUSU6JRWK=
LB2518-MEL Mn\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TUb2lEPTB;MU[uOlA6PCEQvF2= NFuy[HJUSU6JRWK=
NCI-H510A NFTMb3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHHfpA2UUN3ME2xO{4zPDR{IN88US=> NFXPWFNUSU6JRWK=
TE-441-T M{LLeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K4ZWlEPTB;MUeuNlg5PiEQvF2= M3\mb3NCVkeHUh?=
HH M4OxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37NTGlEPTB;MUeuN|k6QSEQvF2= NYHpOYI{W0GQR1XS
LC4-1 NEO1eplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUmyS|RPUUN3ME2xPE4xPjV{IN88US=> M2XhNHNCVkeHUh?=
KARPAS-45 NG\0eY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTOTWM2OD1zOD6xPFQ5KM7:TR?= MXrTRW5ITVJ?
LB1047-RCC NFj2T3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrIc4tKSzVyPUG4MlQ1PTJizszN NYXvNWJtW0GQR1XS
NKM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3kTWM2OD1zOT6zOVUzKM7:TR?= MorDV2FPT0WU
SCLC-21H NG\DOYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLJTWM2OD1{MD6xNlQ3KM7:TR?= NULTU|ZqW0GQR1XS
RS4-11 NHrSXoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LiZWlEPTB;MkCuN|MxQCEQvF2= M1rabnNCVkeHUh?=
ALL-PO NHHJ[5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjsVI9KSzVyPUKwMlgyPDlizszN MVXTRW5ITVJ?
GDM-1 M2XuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LaTmlEPTB;MkKuOVk1PSEQvF2= NWP2fZNzW0GQR1XS
DMS-79 MnjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LreWlEPTB;MkSuOFk{PCEQvF2= MVrTRW5ITVJ?
MPP-89 M{PmOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVSwWVFHUUN3ME2yOU43QDd2IN88US=> NH;Ud41USU6JRWK=
NB10 MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vIe2lEPTB;Mk[uOFY6QSEQvF2= MUPTRW5ITVJ?
LS-513 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\qbGlEPTB;Mk[uPFg1PyEQvF2= MVvTRW5ITVJ?
L-540 NVTDZ|E4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfsTWM2OD1{Nj65NVQ{KM7:TR?= NYjBR|VSW0GQR1XS
ES1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG5cVVOUUN3ME2yO{42OjFizszN M1v0b3NCVkeHUh?=
NTERA-S-cl-D1 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jJXmlEPTB;M{CuOVA6OyEQvF2= M2POeXNCVkeHUh?=
EW-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\uUmlEPTB;M{KuPVQ2PCEQvF2= NInzdWNUSU6JRWK=
Calu-6 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHxZo5FUUN3ME2zN{4yQDV3IN88US=> MoTWV2FPT0WU
CTV-1 M2q2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHtboZKSzVyPUOzMlk4QDlizszN M3zYbnNCVkeHUh?=
YT M{LuTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX5R5dKSzVyPUO4MlUzODlizszN NVf1bYQxW0GQR1XS
TE-6 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\QcWlEPTB;NEGuNlc6QCEQvF2= NHHBPHpUSU6JRWK=
HT-144 NY\n[HhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTRzLkW0PFYh|ryP NFHL[lFUSU6JRWK=
EW-13 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTR{LkK3PVEh|ryP M4HmSHNCVkeHUh?=
KALS-1 M17qXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TrXWlEPTB;NEOuNVMzQSEQvF2= MmnaV2FPT0WU
MOLT-16 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofPTWM2OD12NT6wO|UzKM7:TR?= MUjTRW5ITVJ?
D-336MG NUHFeWM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPqTWM2OD12NT65OVk6KM7:TR?= NUnreVJzW0GQR1XS
TE-11 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rTOmlEPTB;NE[uOlU{KM7:TR?= NGf4TXlUSU6JRWK=
EB2 NIDGbGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjkZXpGUUN3ME20Ok43QTlizszN MlLVV2FPT0WU
SK-N-DZ M{fPdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HTUmlEPTB;NEiuNFk3OSEQvF2= NVHRTmRSW0GQR1XS
SW684 NFewe2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPPe4YyUUN3ME20PE4zPjl3IN88US=> MVLTRW5ITVJ?
EW-18 M2LwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDaPXhKSzVyPUS4MlQ{QTVizszN MULTRW5ITVJ?
RL95-2 NWr0fmd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjLXW95UUN3ME21NE4xPzFizszN MoS5V2FPT0WU
CHP-126 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDtPZFKSzVyPUWwMlg6ODVizszN NEPaXnlUSU6JRWK=
NCI-H1395 M13OV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXITWM2OD13MT63PFM2KM7:TR?= MX\TRW5ITVJ?
TE-15 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fLSmlEPTB;NUKuNlU2PiEQvF2= NIDhT2JUSU6JRWK=
ES4 Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13JbGlEPTB;NUKuPVc4PSEQvF2= Mlq3V2FPT0WU
TE-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFmyelFKSzVyPUWzMlk1PTVizszN Mn7qV2FPT0WU
SIMA NF35e29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rLZ2lEPTB;NUeuN|MyOSEQvF2= NIjNfllUSU6JRWK=
LB647-SCLC MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFT6OXJKSzVyPU[0MlEyQDhizszN NHjlXGNUSU6JRWK=
KY821 M1v3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TlZmlEPTB;NkSuNlU2OiEQvF2= NXPpR4RYW0GQR1XS
LC-2-ad NHXDRWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG3TWM2OD14NT63OlAyKM7:TR?= MkHrV2FPT0WU
KP-N-RT-BM-1 MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTZ4Lk[zOlYh|ryP M2OxR3NCVkeHUh?=
SW872 MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zuXmlEPTB;NkeuOFM5OiEQvF2= MnXSV2FPT0WU
ES5 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTZ5Lk[5Olgh|ryP MnjMV2FPT0WU
SK-NEP-1 M{\4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7JTWM2OD14OD6zPFA{KM7:TR?= NUjUXXBrW0GQR1XS
RPMI-6666 M3nLTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFewZ4ZKSzVyPUexMlA{OiEQvF2= NV\SNJBvW0GQR1XS
UACC-812 NXf3XmgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVKxPGZvUUN3ME23NU4yPjB7IN88US=> Mn[1V2FPT0WU
COLO-829 MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[0TWM2OD15Mj62PVg4KM7:TR?= NXLTbHBJW0GQR1XS
KP-N-YS NYDze3BDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zPXGlEPTB;N{KuO|E{QSEQvF2= NHTaRZpUSU6JRWK=
GI-1 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHOOFhyUUN3ME23N{4zQDZ6IN88US=> Ml7SV2FPT0WU
ETK-1 NIHxOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjpdHFKSzVyPUezMlQ6OzJizszN MoDpV2FPT0WU
LXF-289 NYrmbVVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLxTWM2OD15Mz63Nlkh|ryP M1PsWHNCVkeHUh?=
CAS-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK5bYVwUUN3ME23N{45QDV5IN88US=> M{XhUnNCVkeHUh?=
EW-22 M1XLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLI[IxpUUN3ME23OE44OTF3IN88US=> MYfTRW5ITVJ?
NCI-H2196 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;aSWlEPTB;N{WuOlM4QSEQvF2= NIPiTmZUSU6JRWK=
EoL-1-cell MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\OOHJKSzVyPUixMlY6PjNizszN MWnTRW5ITVJ?
D-247MG M2WyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fEZWlEPTB;OEKuNFI1QCEQvF2= NUjiS4J4W0GQR1XS
Becker MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXBOHVXUUN3ME24Nk4{PDhzIN88US=> NUKybYVQW0GQR1XS
IST-MEL1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vUNGlEPTB;OEKuN|Q5OiEQvF2= MYrTRW5ITVJ?
MDA-MB-134-VI M{nWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTh{LkW5PVYh|ryP NUjuSmRWW0GQR1XS
NCI-H1092 M4LOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH4TWM2OD16ND6wNVk4KM7:TR?= NHzTXnZUSU6JRWK=
KINGS-1 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOwWXlJUUN3ME24Ok4yPjF6IN88US=> MWPTRW5ITVJ?
HCC2218 MkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTh4Lke5NVMh|ryP NUnQPYV{W0GQR1XS
GI-ME-N MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWK3bmtZUUN3ME24O{44Pjl7IN88US=> MVzTRW5ITVJ?
AM-38 M2fJTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HoemlEPTB;OEiuN|k2OyEQvF2= NV\Z[5RqW0GQR1XS
KNS-42 NGDMZpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;kUGtrUUN3ME24PU4yODF6IN88US=> NWrQ[WlSW0GQR1XS
C8166 NHPNbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjmcpRiUUN3ME24PU43OTJ3IN88US=> NHrZWXFUSU6JRWK=
Ramos-2G6-4C10 M3fWR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vPeGlEPTB;OEmuPFcyQSEQvF2= NUTBfmZ2W0GQR1XS
CTB-1 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvqdItwUUN3ME25NE43OzV5IN88US=> MWDTRW5ITVJ?
HCE-4 M1flVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrTbnJKSzVyPUmxMlE{OzZizszN NGjkTZRUSU6JRWK=
NCI-H526 NHv1WFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{G5SmlEPTB;OUKuOFExOyEQvF2= NGnOeXVUSU6JRWK=
ECC4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DlPGlEPTB;OUSuNlU2PSEQvF2= M1:2R3NCVkeHUh?=
NCCIT MkLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDjTWM2OD17NT6zNlkzKM7:TR?= MXvTRW5ITVJ?
MZ7-mel NH\WOmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmK1TWM2OD17NT65NFQh|ryP M{TQWHNCVkeHUh?=
COLO-684 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;ZZY9KSzVyPUm2MlI{QDVizszN MX3TRW5ITVJ?
SU-DHL-1 NEfHUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f5SmlEPTB;OU[uPVg1OiEQvF2= MW\TRW5ITVJ?
SF126 NVfHdGo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;FbWlEPTB;OUeuOVIyPyEQvF2= MU\TRW5ITVJ?
NMC-G1 M4fiNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvUUlhbUUN3ME25PE41PTV2IN88US=> NXnzO45zW0GQR1XS
NB14 M2XuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fZeWlEPTB;OUiuPVIxQCEQvF2= M3rJdXNCVkeHUh?=
VA-ES-BJ NGnFUIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nrcGlEPTB;OUmuOFA2PiEQvF2= NHzZ[npUSU6JRWK=

... 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(配方适用于不溶于水的药物;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