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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RMB 980.11 现货
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客户使用Selleck该产品发表文献37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 MmjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O0b2lEPTB;MD6wO|MxPCEQvF2= NUPDfXBiW0GQR1XS
EM-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTWTWM2OD1yLkC4PFgh|ryP NWOzRnZEW0GQR1XS
MEG-01 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYq5[oJOUUN3ME2wMlA5QTJzIN88US=> M4XsVHNCVkeHUh?=
BV-173 M{TneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnoUlNxUUN3ME2wMlE5PzRizszN MUTTRW5ITVJ?
K-562 M4Llemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP3XY1KSzVyPUCuNlI1OzJizszN M4H1[3NCVkeHUh?=
CGTH-W-1 NHzyWFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwM{izO|Qh|ryP M2HMdXNCVkeHUh?=
ST486 NXq3W4FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHmWXR6UUN3ME2wMlY5PTRizszN Mn;wV2FPT0WU
NCI-H1436 Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3OTmpKSzVyPUCuPVc5ODFizszN MV;TRW5ITVJ?
NOS-1 M1m2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFwNkWzPFMh|ryP NF61R45USU6JRWK=
A498 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjjbnRmUUN3ME2yMlU4OjJ|IN88US=> M1f5XnNCVkeHUh?=
BE-13 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\ZZlhCUUN3ME2yMlYzOTB4IN88US=> MmXTV2FPT0WU
SUP-T1 MofnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnkTWM2OD1|LkiyPVA4KM7:TR?= NEixUIpUSU6JRWK=
NCI-H1770 M13wcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe3W25xUUN3ME21MlU4OjZ{IN88US=> NHrZPVJUSU6JRWK=
IMR-5 NIDRdVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUiwT|NqUUN3ME22MlIzOTR5IN88US=> M4S2R3NCVkeHUh?=
LB2241-RCC M2rxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzGVXdKSzVyPUiuNFc{QDRizszN MkPLV2FPT0WU
TGBC24TKB NXP2T5JJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDCTWM2OD16LkO0NFUzKM7:TR?= MWfTRW5ITVJ?
SCC-15 M2myT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfaTWM2OD1zMD63O|g5KM7:TR?= NV;tSlhpW0GQR1XS
BB49-HNC NHzscpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTzOZdJUUN3ME2xOE4{OzN3IN88US=> MlXDV2FPT0WU
ES7 NUf0[XZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTF2LkezO|kh|ryP M2THWnNCVkeHUh?=
LB2518-MEL MoOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Tze2lEPTB;MU[uOlA6PCEQvF2= NGL6TJJUSU6JRWK=
NCI-H510A MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF60dVhKSzVyPUG3MlI1PDJizszN MnXLV2FPT0WU
TE-441-T M1X0XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\0TWM2OD1zNz6yPFg3KM7:TR?= NXm0VXF{W0GQR1XS
HH MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3H4WmlEPTB;MUeuN|k6QSEQvF2= MoLGV2FPT0WU
LC4-1 M3vob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\DVpZEUUN3ME2xPE4xPjV{IN88US=> MnPpV2FPT0WU
KARPAS-45 NGLEU3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXj[2hZUUN3ME2xPE4yQDR6IN88US=> NHfHeVNUSU6JRWK=
LB1047-RCC MlfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF6LkS0OVIh|ryP MnTOV2FPT0WU
NKM-1 Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH2VYZKSzVyPUG5MlM2PTJizszN MXfTRW5ITVJ?
SCLC-21H NEHKfFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJyLkGyOFYh|ryP M2HqRXNCVkeHUh?=
RS4-11 MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\0SWtKSzVyPUKwMlM{ODhizszN MV3TRW5ITVJ?
ALL-PO MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fMd2lEPTB;MkCuPFE1QSEQvF2= MYXTRW5ITVJ?
GDM-1 NIDSSJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\hRVRKSzVyPUKyMlU6PDVizszN NXTtPJZuW0GQR1XS
DMS-79 NYnyU49mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEntU3RKSzVyPUK0MlQ6OzRizszN M2jifnNCVkeHUh?=
MPP-89 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnITWM2OD1{NT62PFc1KM7:TR?= MXjTRW5ITVJ?
NB10 M1u2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjFb5BKSzVyPUK2MlQ3QTlizszN MoXvV2FPT0WU
LS-513 NXvI[pZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLZOYJKSzVyPUK2Mlg5PDdizszN NFrR[olUSU6JRWK=
L-540 NEP3fWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\EN2lEPTB;Mk[uPVE1OyEQvF2= M4XXSnNCVkeHUh?=
ES1 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTsTpBoUUN3ME2yO{42OjFizszN M4\YenNCVkeHUh?=
NTERA-S-cl-D1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\nSmlEPTB;M{CuOVA6OyEQvF2= MoXVV2FPT0WU
EW-1 NF3HXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\ETWM2OD1|Mj65OFU1KM7:TR?= MnP2V2FPT0WU
Calu-6 M3PZe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPkTWM2OD1|Mz6xPFU2KM7:TR?= NWixT4hiW0GQR1XS
CTV-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\yeGlEPTB;M{OuPVc5QSEQvF2= MVHTRW5ITVJ?
YT NF;hNIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfhPFBKSzVyPUO4MlUzODlizszN NF3yS4VUSU6JRWK=
TE-6 NWXlc5NST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTRzLkK3PVgh|ryP NELGWJhUSU6JRWK=
HT-144 NVrje2p7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\hTWM2OD12MT61OFg3KM7:TR?= M4fn[HNCVkeHUh?=
EW-13 MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXETWM2OD12Mj6yO|kyKM7:TR?= NVr2dItHW0GQR1XS
KALS-1 MnLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELkXYhKSzVyPUSzMlE{OjlizszN M1PtbnNCVkeHUh?=
MOLT-16 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\ncZhKSzVyPUS1MlA4PTJizszN Mn3rV2FPT0WU
D-336MG NX7w[Y5sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmToTWM2OD12NT65OVk6KM7:TR?= MYLTRW5ITVJ?
TE-11 NVfIXHRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR4Lk[1N{DPxE1? Mo\aV2FPT0WU
EB2 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fUN2lEPTB;NE[uOlk6KM7:TR?= NW\KXFc3W0GQR1XS
SK-N-DZ NXvCTVRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnv6TWM2OD12OD6wPVYyKM7:TR?= Ml[zV2FPT0WU
SW684 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TaeWlEPTB;NEiuNlY6PSEQvF2= M1TZ[XNCVkeHUh?=
EW-18 M1fVVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnpT4hSUUN3ME20PE41Ozl3IN88US=> NYnmVFd4W0GQR1XS
RL95-2 M4DTbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTVyLkC3NUDPxE1? M3nGPXNCVkeHUh?=
CHP-126 NULuc28xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTVyLki5NFUh|ryP M2Dud3NCVkeHUh?=
NCI-H1395 NYLIUZViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDOSYJKSzVyPUWxMlc5OzVizszN M2LqVXNCVkeHUh?=
TE-15 NFzSTZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHKWG92UUN3ME21Nk4zPTV4IN88US=> M3u0WHNCVkeHUh?=
ES4 NIHLXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKwNJlEUUN3ME21Nk46Pzd3IN88US=> MYLTRW5ITVJ?
TE-1 NHLWRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTV|Lkm0OVUh|ryP NI\FXHVUSU6JRWK=
SIMA Mk\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\3W41KSzVyPUW3MlM{OTFizszN MX7TRW5ITVJ?
LB647-SCLC Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTZ2LkGxPFgh|ryP NGizRndUSU6JRWK=
KY821 M{jQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK1emZpUUN3ME22OE4zPTV{IN88US=> MmTCV2FPT0WU
LC-2-ad NY\3dmJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzvTWM2OD14NT63OlAyKM7:TR?= NFvhe4pUSU6JRWK=
KP-N-RT-BM-1 NV;TOlJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\3PWlEPTB;Nk[uOlM3PiEQvF2= MnTOV2FPT0WU
SW872 MkS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHxTWM2OD14Nz60N|gzKM7:TR?= M13DWnNCVkeHUh?=
ES5 NUj0SIxiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmniTWM2OD14Nz62PVY5KM7:TR?= NWrWcXRXW0GQR1XS
SK-NEP-1 M1XBPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3q4O2lEPTB;NkiuN|gxOyEQvF2= NIqxTYFUSU6JRWK=
RPMI-6666 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETWVmxKSzVyPUexMlA{OiEQvF2= NFvkUotUSU6JRWK=
UACC-812 NVTSepB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rGdWlEPTB;N{GuNVYxQSEQvF2= MWnTRW5ITVJ?
COLO-829 M1fud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT5TIpJUUN3ME23Nk43QTh5IN88US=> NGLsPG5USU6JRWK=
KP-N-YS NUfmTGtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vFSWlEPTB;N{KuO|E{QSEQvF2= M37RfXNCVkeHUh?=
GI-1 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTd|LkK4Olgh|ryP NHGycItUSU6JRWK=
ETK-1 NYG2TooyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTd|LkS5N|Ih|ryP MXzTRW5ITVJ?
LXF-289 NFPXWoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nocWlEPTB;N{OuO|I6KM7:TR?= NX;3U2VnW0GQR1XS
CAS-1 NID2XXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonJTWM2OD15Mz64PFU4KM7:TR?= M4j1dHNCVkeHUh?=
EW-22 NUW5UmNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\MTWM2OD15ND63NVE2KM7:TR?= NYPUfINJW0GQR1XS
NCI-H2196 NVO3Zm9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fNUGlEPTB;N{WuOlM4QSEQvF2= MYrTRW5ITVJ?
EoL-1-cell NGXJT3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRThzLk[5OlMh|ryP NUntWY1vW0GQR1XS
D-247MG NUjte4hRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXrTWM2OD16Mj6wNlQ5KM7:TR?= NWjzU2lXW0GQR1XS
Becker M4W5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4iyZWlEPTB;OEKuN|Q5OSEQvF2= NVjzPJVoW0GQR1XS
IST-MEL1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnUbXloUUN3ME24Nk4{PDh{IN88US=> NHLoendUSU6JRWK=
MDA-MB-134-VI NYjpRpFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrLbohbUUN3ME24Nk42QTl4IN88US=> NGXmfnhUSU6JRWK=
NCI-H1092 MoPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfzTndrUUN3ME24OE4xOTl5IN88US=> Mk\XV2FPT0WU
KINGS-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTh4LkG2NVgh|ryP NX25e3E5W0GQR1XS
HCC2218 M4\qfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XHWWlEPTB;OE[uO|kyOyEQvF2= M1LtWHNCVkeHUh?=
GI-ME-N NFjTcZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3m4b2lEPTB;OEeuO|Y6QSEQvF2= NFntWlRUSU6JRWK=
AM-38 M1i3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XnUmlEPTB;OEiuN|k2OyEQvF2= MkD4V2FPT0WU
KNS-42 M{PWemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTh7LkGwNVgh|ryP NIDHOYdUSU6JRWK=
C8166 Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jv[GlEPTB;OEmuOlEzPSEQvF2= NGHGOFBUSU6JRWK=
Ramos-2G6-4C10 M4\SRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTh7Lki3NVkh|ryP MXzTRW5ITVJ?
CTB-1 M4nuU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrES45KSzVyPUmwMlY{PTdizszN NVnSRWttW0GQR1XS
HCE-4 NH\oZ5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HYdGlEPTB;OUGuNVM{PiEQvF2= NGH3OXlUSU6JRWK=
NCI-H526 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknZTWM2OD17Mj60NVA{KM7:TR?= M1jKVXNCVkeHUh?=
ECC4 M1nsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTl2LkK1OVUh|ryP M4rx[nNCVkeHUh?=
NCCIT NFXNSIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjNW3M5UUN3ME25OU4{Ojl{IN88US=> MorrV2FPT0WU
MZ7-mel M4\VUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfL[HVKSzVyPUm1MlkxPCEQvF2= NXvie|ZKW0GQR1XS
COLO-684 NYLPN5N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;wbmxUUUN3ME25Ok4zOzh3IN88US=> MlP1V2FPT0WU
SU-DHL-1 NGjzdI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHHN4VKSzVyPUm2Mlk5PDJizszN MUnTRW5ITVJ?
SF126 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\Lb2lEPTB;OUeuOVIyPyEQvF2= MXnTRW5ITVJ?
NMC-G1 M4C5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTzTYN[UUN3ME25PE41PTV2IN88US=> NETUbVJUSU6JRWK=
NB14 M1THSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q0Z2lEPTB;OUiuPVIxQCEQvF2= NYT6OFBkW0GQR1XS
VA-ES-BJ NIPjbnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXDTWM2OD17OT60NFU3KM7:TR?= NUfvPYNzW0GQR1XS

... Click to View More Cell Line Experimental Data

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:

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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
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03862768 Not yet recruiting Gastrointestinal Stromal Tumors|Surgery Shanghai Zhongshan Hospital July 2019 Not Applicable
NCT03862768 Not yet recruiting Gastrointestinal Stromal Tumors|Surgery Shanghai Zhongshan Hospital July 2019 Not Applicable
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03802084 Not yet recruiting Desmoid Tumor Yonsei University April 2019 Phase 1|Phase 2
NCT03802084 Not yet recruiting Desmoid Tumor Yonsei University April 2019 Phase 1|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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID