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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客户购买Selleck的此次产品后发表的文献35篇:

客户使用该产品的6个实验数据:

  • Ba/F3-p210T315I cells were treated with indicated concentrations of imatinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

    FASEB J 2011 25, 3661-3673. Imatinib (STI571) purchased from Selleck.

    Targeting KITLG through c-KIT inhibition using Imatinib; one representative experiment is shown (n = 4).

    Oncotarget, 2016, 7(34):54583-54595. Imatinib (STI571) purchased from Selleck.

  •  

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with imatinib. K562 cells (a and c) and MEG-01 cells (b and d) were incubated at 37 ◦C for 15 min with imatinib transport buffer, and then incubated with 0.5 Ci of [3H] thymidine or [3H] cytarabine for an additional 5 min in presence of imatinib. Cells were then washed 3 times, lysed and radioactivity associated to cell pellets was quantified. DMSO, dimethylsulfoxide; DPD, dipyridamole.

    Leukemia Res 2012 36, 1311-1314. Imatinib (STI571) purchased from Selleck.

    ZFX regulates imatinib sensitivity and PI3K/Akt signaling pathway in CML cells. Viability of cells transfected with si-ZFX at the indicated doses of imatinib for 24 h (a). Colonies of leukemia cells and imatinib-resistant cells transfected with si-ZFX following treatment with imatinib for 10 days (b). Western blot analysis of Akt, p-Akt, CyclinD1, CyclinE1, Bcl-2, and Caspase-3 in K562 and K562/G01 cells transfected with si-ZFX for 2 days (c). The relative densities of proteins were quantified and normalized to b-Actin (d). Values represented the mean ± SD data from experiments in triplicate. *P\0.05 and **P\0.01

    Cell Biochem Biophys, 2016, 74(2):277-83. Imatinib (STI571) purchased from Selleck.

  • Cell Viability assay results. A2C12, BetaD5, GammaA3, GammaD12, A549, CaCo2, HepG2 cell lines were treated with imatinib mesylate for 24h and 96h.

    Dr. Thomas Kruwel of Fraunhofer. Imatinib (STI571) purchased from Selleck.

    A. Viability curve for the c-Kit mutant MelMS melanoma cell line treated with increasing concentrations of imatinib for 72h (relative to DMSO-treated controls; mean ±sd; n=3) B. MelMS melanoma cells were treated with 50nM imatinib for 24h. The effects on c-Kit, ERK and AKT activation were determined by immunoblotting.

    Dr. Helen Rizos from the university of Sydney. Imatinib (STI571) purchased from Selleck.

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 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjmTWM2OD1yLkC3N|A1KM7:TR?= MXPTRW5ITVJ?
EM-2 NHywXFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\GOWJKSzVyPUCuNFg5QCEQvF2= M1zyRnNCVkeHUh?=
MEG-01 NXS5dHZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvVTWM2OD1yLkC4PVIyKM7:TR?= MWPTRW5ITVJ?
BV-173 M4PkfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXflO3VKUUN3ME2wMlE5PzRizszN NVrmUGF[W0GQR1XS
K-562 NHHZTZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwMkK0N|Ih|ryP NHjwdZZUSU6JRWK=
CGTH-W-1 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj2TWM2OD1yLkO4N|c1KM7:TR?= MVnTRW5ITVJ?
ST486 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XZc2lEPTB;MD62PFU1KM7:TR?= M4XneXNCVkeHUh?=
NCI-H1436 NFX0T25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[3Zno2UUN3ME2wMlk4QDBzIN88US=> NV\SZ3A6W0GQR1XS
NOS-1 M3fXSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr4c4ZKSzVyPUGuOlU{QDNizszN M1PCWHNCVkeHUh?=
A498 NH7yfGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJwNUeyNlMh|ryP MkO1V2FPT0WU
BE-13 NWHLNHRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDXVFRKSzVyPUKuOlIyODZizszN NGOzdlZUSU6JRWK=
SUP-T1 M4Ljcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED0[mNKSzVyPUOuPFI6ODdizszN MVTTRW5ITVJ?
NCI-H1770 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;aXWlEPTB;NT61O|I3OiEQvF2= MlOxV2FPT0WU
IMR-5 NFjrPZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTZwMkKxOFch|ryP M3HaZ3NCVkeHUh?=
LB2241-RCC NWXteoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HCOWlEPTB;OD6wO|M5PCEQvF2= NWXnfI5RW0GQR1XS
TGBC24TKB MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O5XGlEPTB;OD6zOFA2OiEQvF2= NVi5U3ZCW0GQR1XS
SCC-15 NX3o[YtZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTFyLke3PFgh|ryP MmLaV2FPT0WU
BB49-HNC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLNWHVWUUN3ME2xOE4{OzN3IN88US=> NYjiV3RbW0GQR1XS
ES7 NVGyPFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTF2LkezO|kh|ryP NFjZPXNUSU6JRWK=
LB2518-MEL M2Tqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTF4Lk[wPVQh|ryP NWjMe41jW0GQR1XS
NCI-H510A MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF5LkK0OFIh|ryP NIPEVGJUSU6JRWK=
TE-441-T NID2epdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfTXWpHUUN3ME2xO{4zQDh4IN88US=> NET3TJFUSU6JRWK=
HH Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLSTWM2OD1zNz6zPVk6KM7:TR?= Mn25V2FPT0WU
LC4-1 MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPJOpl6UUN3ME2xPE4xPjV{IN88US=> MYnTRW5ITVJ?
KARPAS-45 NWDNRnh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvWTWM2OD1zOD6xPFQ5KM7:TR?= MV3TRW5ITVJ?
LB1047-RCC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m1d2lEPTB;MUiuOFQ2OiEQvF2= NGrLN5pUSU6JRWK=
NKM-1 NV;tdIN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF7LkO1OVIh|ryP MmG2V2FPT0WU
SCLC-21H MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX62cGMxUUN3ME2yNE4yOjR4IN88US=> NGjjb|dUSU6JRWK=
RS4-11 M4Lqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;JU2dFUUN3ME2yNE4{OzB6IN88US=> NUmyWIxPW0GQR1XS
ALL-PO NUTFclF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH6c3ByUUN3ME2yNE45OTR7IN88US=> M2GxNHNCVkeHUh?=
GDM-1 NWXFelN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;Yd5hxUUN3ME2yNk42QTR3IN88US=> NHr3U4FUSU6JRWK=
DMS-79 MlnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nQOGlEPTB;MkSuOFk{PCEQvF2= NWLrOnF1W0GQR1XS
MPP-89 M3TDZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP4SoxKSzVyPUK1MlY5PzRizszN MWrTRW5ITVJ?
NB10 Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJ4LkS2PVkh|ryP Ml\tV2FPT0WU
LS-513 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\n[|VlUUN3ME2yOk45QDR5IN88US=> MUjTRW5ITVJ?
L-540 M1zaemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfXZ3FvUUN3ME2yOk46OTR|IN88US=> MXTTRW5ITVJ?
ES1 NISzW2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\6OWFXUUN3ME2yO{42OjFizszN M1X2PXNCVkeHUh?=
NTERA-S-cl-D1 M4jDVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTNyLkWwPVMh|ryP NFr3elRUSU6JRWK=
EW-1 Ml60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\RbGdOUUN3ME2zNk46PDV2IN88US=> NE[yR|FUSU6JRWK=
Calu-6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN|LkG4OVUh|ryP NGT3PZFUSU6JRWK=
CTV-1 NYTuVo5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTN|Lkm3PFkh|ryP Mkj0V2FPT0WU
YT NFvn[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDqTWM2OD1|OD61NlA6KM7:TR?= MVXTRW5ITVJ?
TE-6 NWfUWGRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWK0OWduUUN3ME20NU4zPzl6IN88US=> NXz2THZiW0GQR1XS
HT-144 M1nseGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDmSINyUUN3ME20NU42PDh4IN88US=> NYDIUGY4W0GQR1XS
EW-13 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn1N3JPUUN3ME20Nk4zPzlzIN88US=> NH\nbWJUSU6JRWK=
KALS-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjQXJdKSzVyPUSzMlE{OjlizszN NFj4N|hUSU6JRWK=
MOLT-16 NXnrPIF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlewTWM2OD12NT6wO|UzKM7:TR?= M2DZRXNCVkeHUh?=
D-336MG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCTWM2OD12NT65OVk6KM7:TR?= M1jNTnNCVkeHUh?=
TE-11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\MfY5kUUN3ME20Ok43PTNizszN MVLTRW5ITVJ?
EB2 Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGH6NlNKSzVyPUS2MlY6QSEQvF2= M1rqXXNCVkeHUh?=
SK-N-DZ NYf0TWVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zoTWlEPTB;NEiuNFk3OSEQvF2= MUnTRW5ITVJ?
SW684 NHz6XFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTR6LkK2PVUh|ryP NFrLOHJUSU6JRWK=
EW-18 M2rqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrFV4hKSzVyPUS4MlQ{QTVizszN NYPHe5pLW0GQR1XS
RL95-2 NFnTfmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHyTWM2OD13MD6wO|Eh|ryP MkTuV2FPT0WU
CHP-126 NViyNZJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[1T2pFUUN3ME21NE45QTB3IN88US=> NYfrWY5EW0GQR1XS
NCI-H1395 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHweWhKSzVyPUWxMlc5OzVizszN NUi0U5ZrW0GQR1XS
TE-15 NVzVblZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn32TWM2OD13Mj6yOVU3KM7:TR?= M3fDT3NCVkeHUh?=
ES4 NH[5SW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTV{Lkm3O|Uh|ryP NWPtdXRuW0GQR1XS
TE-1 M{\HXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXuwSHYxUUN3ME21N{46PDV3IN88US=> MmfpV2FPT0WU
SIMA M3PpTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6yTWM2OD13Nz6zN|EyKM7:TR?= NFXYSIFUSU6JRWK=
LB647-SCLC MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXQO5Z7UUN3ME22OE4yOTh6IN88US=> MlrJV2FPT0WU
KY821 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHId5B6UUN3ME22OE4zPTV{IN88US=> M2KwcHNCVkeHUh?=
LC-2-ad MnX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrq[2p{UUN3ME22OU44PjBzIN88US=> MWPTRW5ITVJ?
KP-N-RT-BM-1 NIjQRmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;GTWM2OD14Nj62N|Y3KM7:TR?= NUTLe5BbW0GQR1XS
SW872 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\xU3RuUUN3ME22O{41Ozh{IN88US=> Mme0V2FPT0WU
ES5 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\mTWM2OD14Nz62PVY5KM7:TR?= NILQTGJUSU6JRWK=
SK-NEP-1 M1XsUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzs[mVKSzVyPU[4MlM5ODNizszN M1r0OHNCVkeHUh?=
RPMI-6666 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HnXmlEPTB;N{GuNFMzKM7:TR?= NIezS4JUSU6JRWK=
UACC-812 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TDfmlEPTB;N{GuNVYxQSEQvF2= MUjTRW5ITVJ?
COLO-829 NHXjTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe3UGVKSzVyPUeyMlY6QDdizszN NETSS|VUSU6JRWK=
KP-N-YS NYfDbYVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr1VY9KSzVyPUeyMlcyOzlizszN NWXYSnVQW0GQR1XS
GI-1 MmDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrqN45FUUN3ME23N{4zQDZ6IN88US=> M2jVO3NCVkeHUh?=
ETK-1 MnXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXPTWM2OD15Mz60PVMzKM7:TR?= MoLoV2FPT0WU
LXF-289 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVi0O3BnUUN3ME23N{44OjlizszN NGnibmhUSU6JRWK=
CAS-1 NGXJfIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHftVZdKSzVyPUezMlg5PTdizszN MlPNV2FPT0WU
EW-22 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH5RYVKSzVyPUe0MlcyOTVizszN NFT0fFNUSU6JRWK=
NCI-H2196 M3LGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zFN2lEPTB;N{WuOlM4QSEQvF2= MVLTRW5ITVJ?
EoL-1-cell M1HDVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLlTWM2OD16MT62PVY{KM7:TR?= Mk\HV2FPT0WU
D-247MG Ml32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qyS2lEPTB;OEKuNFI1QCEQvF2= M2jVTnNCVkeHUh?=
Becker MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTh{LkO0PFEh|ryP NEPRN3FUSU6JRWK=
IST-MEL1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTh{LkO0PFIh|ryP NW\rWHlpW0GQR1XS
MDA-MB-134-VI MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2n4R2lEPTB;OEKuOVk6PiEQvF2= MWDTRW5ITVJ?
NCI-H1092 NUjSZnM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPnO3NKSzVyPUi0MlAyQTdizszN NFrKVVdUSU6JRWK=
KINGS-1 M{HTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vnOGlEPTB;OE[uNVYyQCEQvF2= M{L0e3NCVkeHUh?=
HCC2218 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLLZYV4UUN3ME24Ok44QTF|IN88US=> NIHhTZFUSU6JRWK=
GI-ME-N NYXoXoM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3pNok4UUN3ME24O{44Pjl7IN88US=> NYr0TYF1W0GQR1XS
AM-38 Mo[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTh6LkO5OVMh|ryP NFHJTY9USU6JRWK=
KNS-42 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojuTWM2OD16OT6xNFE5KM7:TR?= MkfyV2FPT0WU
C8166 NEn3fmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnv[otKSzVyPUi5MlYyOjVizszN M4fJXnNCVkeHUh?=
Ramos-2G6-4C10 M1XrdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLrTWM2OD16OT64O|E6KM7:TR?= NFvNNXVUSU6JRWK=
CTB-1 NIS2XZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofDTWM2OD17MD62N|U4KM7:TR?= MknWV2FPT0WU
HCE-4 MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M372dGlEPTB;OUGuNVM{PiEQvF2= MW\TRW5ITVJ?
NCI-H526 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTl{LkSxNFMh|ryP MV\TRW5ITVJ?
ECC4 NHHOSGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDI[lZNUUN3ME25OE4zPTV3IN88US=> M1jaTHNCVkeHUh?=
NCCIT M{XzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTl3LkOyPVIh|ryP MonjV2FPT0WU
MZ7-mel M1Tnc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[xfZE4UUN3ME25OU46ODRizszN MWfTRW5ITVJ?
COLO-684 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfy[G9QUUN3ME25Ok4zOzh3IN88US=> MoLnV2FPT0WU
SU-DHL-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTl4Lkm4OFIh|ryP NUC3dG1[W0GQR1XS
SF126 NVrmbIpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPUZldPUUN3ME25O{42OjF5IN88US=> Mnm4V2FPT0WU
NMC-G1 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW0TWM2OD17OD60OVU1KM7:TR?= NHzjT3RUSU6JRWK=
NB14 M2TGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTl6LkmyNFgh|ryP MULTRW5ITVJ?
VA-ES-BJ MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTRTWM2OD17OT60NFU3KM7:TR?= MnT6V2FPT0WU

... 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:

[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
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
NCT03343600 Recruiting Patients Who Have Received Allo-HSCT National Taiwan University Hospital|Far Eastern Memorial Hospital|Tri-Service General Hospital|National Cheng-Kung University Hospital|Hualien Tzu Chi General Hospital November 9 2017 Phase 2
NCT00137111 Active not recruiting Lymphoblastic Leukemia Acute St. Jude Children''s Research Hospital|National Cancer Institute (NCI) July 8 2000 Phase 3
NCT01343173 Completed Chronic Myeloid Leukaemia University Hospital Bordeaux April 6 2011 Not Applicable
NCT03214718 Not yet recruiting Chronic Myeloid Leukemia Patients Assiut University August 5 2017 Not Applicable
NCT01319981 Active not recruiting Leukemia M.D. Anderson Cancer Center|Spectrum Pharmaceuticals Inc March 5 2013 Phase 2
NCT02812693 Withdrawn Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma Joanne Jeter|National Cancer Institute (NCI)|Merck Ltd.|Ohio State University Comprehensive Cancer Center November 4 2016 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