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受注：045-509-1970 |
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化学情報
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Synonyms | CGP-57148B,STI571 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C29H31N7O.CH4SO3 |
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| 分子量 | 589.71 | CAS No. | 220127-57-1 | |
| Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (169.57 mM) | |
| Water | 100 mg/mL (169.57 mM) | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Imatinib Mesylate 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. Imatinib Mesylate (STI571) induces autophagy. |
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| in vitro | 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] |
| in vivo | 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] |
プロトコル(参考用のみ)
| キナーゼアッセイ | PDGF receptor kinase activity | |
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| 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. | ||
| 細胞アッセイ | 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. |
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| 動物実験 | 動物モデル | SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female). |
| 投薬量 | 70 or 100 mg/kg | |
| 投与方法 | Administered via i.p. | |
参考
カスタマーフィードバック
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Data from [Leukemia, 2013, 27, 932-40]
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Data from [Cell Death Dis, 2011, 2, e170]
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Data from [FASEB J, 2011, 25, 3661-3673]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Host-functionalization of macrin nanoparticles to enable drug loading and control tumor-associated macrophage phenotype [ Front Immunol, 2024, 15:1331480] | PubMed: 38545103 |
| Sorafenib induces muscle wasting by disrupting the activity of distinct chromatin regulators [ bioRxiv, 2024, 10.1101/2024.01.04.574149] | PubMed: none |
| Cancer stem cell assay-guided chemotherapy improves survival of patients with recurrent glioblastoma in a randomized trial [ Cell Rep Med, 2023, 4(5):101025] | PubMed: 37137304 |
| ABL1 kinase as a tumor suppressor in AML1-ETO and NUP98-PMX1 leukemias [ Blood Cancer J, 2023, 13(1):42] | PubMed: 36959186 |
| Type H vessel/platelet-derived growth factor receptor β+ perivascular cell disintegration is involved in vascular injury and bone loss in radiation-induced bone damage [ Cell Prolif, 2023, e13406.] | PubMed: 36694343 |
| Transformation of primary murine peritoneal mast cells by constitutive KIT activation is accompanied by loss of Cdkn2a/Arf expression [ Front Immunol, 2023, 14:1154416] | PubMed: 37063827 |
| Connexin 43-modified bone marrow stromal cells reverse the imatinib resistance of K562 cells via Ca 2+ -dependent gap junction intercellular communication [ Chin Med J (Engl), 2023, 136(2):194-206] | PubMed: 36801891 |
| N6-methyl-2'-deoxyadenosine promotes self-renewal of BFU-E progenitor in erythropoiesis [ iScience, 2023, 26(6):106924] | PubMed: 37283807 |
| I13 overrides resistance mediated by the T315I mutation in chronic myeloid leukemia by direct BCR-ABL inhibition [ Front Pharmacol, 2023, 14:1183052] | PubMed: 37124196 |
| Unraveling the Mechanisms of Sensitivity to Anti-FGF Therapies in Imatinib-Resistant Gastrointestinal Stromal Tumors (GIST) Lacking Secondary KIT Mutations [ Cancers (Basel), 2023, 15(22)5354] | PubMed: 38001614 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。