Imatinib Mesylate (STI571)

製品コードS1026 別名:CGP-57148B, ST-1571 Mesylate

Imatinib Mesylate (STI571)化学構造

分子量(MW):589.71

Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.

サイズ 価格(税別) 在庫  
In DMSO JPY 33700 あり
JPY 18100 あり
JPY 34700 あり
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バルク問合せ

文献中Selleckの製品使用例(54)

製品安全説明書

Bcr-Abl阻害剤の選択性比較

生物活性

製品説明 Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.
ターゲット
PDGFR [1]
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
体外試験

In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. [1] Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. [2] Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. [3] A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPwTWM2OD13MDFOwG0> NFjNZXUzPTh4M{KzNi=>
Hep G2 M3LSNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkGxTWM2OD1|MTFOwG0> NInrZYszPTh4M{KzNi=>
DU145 NXjjcIlCS2WubDDWbYFjcWyrdImgRZN{[Xl? NHXwb3UzOOLCid88US=> MUm2MVczKGh? M3;xfIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= NF7ZUJgzPTd6Nk[1Oi=>
PC3  NWHHcYNqS2WubDDWbYFjcWyrdImgRZN{[Xl? MVeyNQKBkc7:TR?= NGPBN403NTd{IHi= M3LJbIlv[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= MoXPNlU4QDZ4NU[=
DU145 NXnKVHhQSXCxcITvd4l{KEG|c3H5 NI\ITGkzOOLCid88US=> NYHCXIFCPDhxN{KgbC=> MlLRbY5lfWOnczDj[YxtKGSnYYToJIJ6KGGyb4D0c5Nqew>? NYHNemdZOjV5OE[2OVY>
PC3  M{TvfWFxd3C2b4Ppd{BCe3OjeR?= MYiyNQKBkc7:TR?= NGLEeVA1QC95MjDo NH;VVohqdmO{ZXHz[ZMh[2WubDDzeZJ3cX[jbB?= NHPJVFMzPTd6Nk[1Oi=>
MCF-7 NYKwTYFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLBUoUyOCEQvF2= NIGwRW01QCCq M37QWIJtd2OtczDj[YxtKHC{b3zp[oVz[XSrb36gbY5kemWjc3WgbY5lfWOnZDDifUBDUjOc NGXmR2EzPTJ5NECzOC=>
K-562  NEHKW2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLGeXpKSzVyPUGg{txO NHjrWnczPTJ|OU[2Ni=>
K562  M1HtcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vUO2lEPTB;MD61xsDPxE1? MlTYNlQ6Ozl2MUi=
K562r MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\UTWM2OD1zMNMg{txO MWmyOFk{QTRzOB?=
K562 NWHYdo85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\yRZhGSzVyPUCuNFkh|ryP Ml;uNVY3Pzh2MUS=
K562 NHjRepFEgXSxdH;4bYNqfHliQYPzZZk> M2r1RVI1KGh? NGfPUINKSzVyPUCuNlEh|ryP MlPSNlIxODB{MEe=
MCF-7 MYXDfZRwfG:6aXPpeJkhSXO|YYm= Mo\ZNlQhcA>? MYPJR|UxRTBwOEOg{txO M2HWdFIzODByMkC3
MDA-MB-23 M3juSmN6fG:2b4jpZ4l1gSCDc4PhfS=> MoftNlQhcA>? MkizTWM2OD1zLkig{txO MlfwNlIxODB{MEe=
GIST882 M{O5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXHPVYhcA>? NXXTe5V3UUN3ME2xMlch|ryP MlK0NlQ6ODB{MUK=

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アッセイ
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 S䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖

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-ac䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 

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䲧疝Ỵ疞㧀疜

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. 䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뾠Ղ䐺

28435223
体内試験 Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. [5] In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. [6]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

PDGF receptor kinase activity:

PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
細胞試験: [3]
- 合併
  • 細胞株: BON-1 cells and NCI-H727 cells
  • 濃度: ~100 μM
  • 反応時間: 48 hours
  • 実験の流れ: BON-1 cells and NCI-H727 cells are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 hours (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.
    (参考用のみ)
動物試験:[5]
- 合併
  • 動物モデル: SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
  • 製剤: Imatinib is diluted in water.
  • 投薬量: 70 or 100 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 118 mg/mL (200.09 mM)
Water 118 mg/mL (200.09 mM)
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 589.71
化学式

C29H31N7O.CH4SO3

CAS No. 220127-57-1
保管
in solvent
別名 CGP-57148B, ST-1571 Mesylate

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02687425 Unknown status Drug: Pioglitazone|Drug: imatinib mesylate Leukemia Myelogenous Chronic BCR-ABL Positive Meng Li|Tongji Hospital February 2016 Phase 2
NCT02303899 Unknown status Drug: Gemcitabine|Drug: Imatinib mesylate Mesothelioma Malignant Istituto Clinico Humanitas November 2014 Phase 2
NCT01898377 Active not recruiting Drug: Imatinib mesylate Mycophenolate mofetil Chronic Graft-versus-host Disease Seoul National University Hospital August 2013 Phase 2
NCT02891395 Completed Drug: Imatinib Mesylate and Nilotinib Graft Versus Host Disease University Hospital Lille|Novartis December 24 2012 Phase 2

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID