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.

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文献中の使用例(31)

カスタマーフィードバック(6)

  • THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.

    Leukemia 2013 27, 932-40. Imatinib Mesylate (STI571) purchased from Selleck.

    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 Mesylate (STI571) purchased from Selleck.

  • Inhibition of ER stress response protects against CBD-induced cell death. (b) LX-2 cells were treated with 5 μM CBD in serum-free media for 8 h in the presence or absence of 10 μM imatinib to inhibit ER stress. Expression of PARP, CHOP, and phospho-JNK was determined by western blot analysis and is presented as fold over vehicle.E.M. for n = four independent experiments. (c) Acid phosphatase activity was used to measure LX-2 cell viability following treatment with CBD and imatinib as in (b).

    Cell death dis 2011 2, e170. Imatinib Mesylate (STI571) purchased from Selleck.

    (a) Cell viability was measured by MTT assay after drug treatment. Results are shown as mean ± SD of at least three independent experiments. (b) Indicated cells were exposed to 0.3 μM imatinib for 3 h or 10 μM Y‐632 for 12 h and analyzed by Western blot.

    Cancer Sci, 2016, 107(6):782-90. Imatinib Mesylate (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-Institute for Toxicology and Experimental Medicine. Imatinib Mesylate (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 Mesylate (STI571) purchased from Selleck.

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  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTVyIN88US=> M1fnb|I2QDZ|MkOy
Hep G2 NXjw[5hET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTNzIN88US=> NETBOJczPTh4M{KzNi=>
DU145 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2CwXVIx6oDLzszN NGjGRms3NTd{IHi= MoC0[IVkemWjc3XzJINmdGxidnnhZoltcXS7 NYeyd5ZkOjV5OE[2OVY>
PC3  NIXvVGRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWmyNQKBkc7:TR?= NUO1O5NvPi15MjDo NYXlVoFqcW6lcnXhd4V{KGOnbHygeoli[mmuaYT5 M{W2NVI2Pzh4NkW2
DU145 M1;MPGFxd3C2b4Ppd{BCe3OjeR?= NH7Lb3UzOOLCid88US=> MmTSOFgwPzJiaB?= M1HERolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCjcH;weI9{cXN? NX3vNIF1OjV5OE[2OVY>
PC3  MWHBdI9xfG:|aYOgRZN{[Xl? MUKyNQKBkc7:TR?= NEn2Oo41QC95MjDo NU\vfJVRcW6lcnXhd4V{KGOnbHygd5Vzfmm4YXy= M1Syd|I2Pzh4NkW2
MCF-7 NUK4NmFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3iUI1KOTBizszN NVe3TXdkPDhiaB?= MVPicI9kc3NiY3XscEBxem:uaX\ldoF1cW:wIHnuZ5Jm[XOnIHnu[JVk\WRiYomgRmo{Yg>? NHf1XXkzPTJ5NECzOC=>
K-562  MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV2yNIdzUUN3ME2xJO69VQ>? NGjNd2wzPTJ|OU[2Ni=>
K562  MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rKV2lEPTB;MD61xsDPxE1? M1LSWVI1QTN7NEG4
K562r NHX4[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW3cFhYUUN3ME2xNOKh|ryP NYPXUmdvOjR7M{m0NVg>
K562 M1PPRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED6Zo9GSzVyPUCuNFkh|ryP NFruT3UyPjZ5OESxOC=>
K562 MXPDfZRwfG:6aXPpeJkhSXO|YYm= MV[yOEBp M2jSOGlEPTB;MD6yNUDPxE1? M4\ie|IzODByMkC3
MCF-7 MoDhR5l1d3SxeHnjbZR6KEG|c3H5 Mme4NlQhcA>? NX7xW2Y{UUN3ME2wMlg{KM7:TR?= MkXYNlIxODB{MEe=
MDA-MB-23 M3\Ed2N6fG:2b4jpZ4l1gSCDc4PhfS=> M2ju[|I1KGh? NVzPcGdjUUN3ME2xMlgh|ryP NWHXdYt[OjJyMECyNFc>
GIST882 NIr5RoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWi5OkBp MXfJR|UxRTFwNzFOwG0> MmnSNlQ6ODB{MUK=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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]
+ 展開

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]
+ 展開
  • 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]
+ 展開
  • 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
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
Saline
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 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 (g) = 濃度 (mol/L) x 体積 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT00044304 Recruiting Hypereosinophilic Syndrome National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 22, 2002 Phase 2
NCT02644525 Not yet recruiting Loaisis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) December 21, 2015 Phase 2
NCT03007147 Not yet recruiting B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|BCR-ABL1 Fusion Protein Expression|Minimal Residual Disease|Philadelphia Chromosome Positive|T Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia Childrens Oncology Group|National Cancer Institute (NCI) July 2017 Phase 3
NCT03023046 Not yet recruiting Adult Acute Lymphoblastic Leukemia|Adult Lymphoblastic Lymphoma|CD20 Positive|Philadelphia Chromosome Positive University of Washington|National Cancer Institute (NCI) February 2017 Phase 2
NCT02538926 Not yet recruiting B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T Lymphoblastic Leukemia/Lymphoma|Refractory B Lymphoblastic Lymphoma|Refractory T Lymphoblastic Lymphoma|T Acute Lymphoblastic Leukemia|T Lymphoblastic Lymphoma University of Washington|National Cancer Institute (NCI) January 2017 Phase 2
NCT02812693 Recruiting 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 2016 Phase 1|Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

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。

  • * 必須

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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