Imatinib Mesylate

製品コードS1026 バッチS102605

印刷

化学情報

Chemical Structure 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
分子量 589.71 CAS No. 220127-57-1
Solubility (25°C)* 体外 DMSO 118 mg/mL (200.09 mM)
Water 118 mg/mL (200.09 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

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.
in vitro

In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib Mesylate inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. [1] This compound 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] It 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 this chemical 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 Mesylate 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, this compound 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
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 this compound 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 this compound. 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.
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

  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC42257/
  • https://pubmed.ncbi.nlm.nih.gov/10910906/
  • https://pubmed.ncbi.nlm.nih.gov/17200360/
  • https://pubmed.ncbi.nlm.nih.gov/22161019/
  • https://pubmed.ncbi.nlm.nih.gov/15499612/
  • https://pubmed.ncbi.nlm.nih.gov/19754668/

カスタマーフィードバック

Data from [Leukemia, 2013, 27, 932-40]

Data from [Cell Death Dis, 2011, 2, e170]

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：

Tuft cells restrain intestinal type 2 immunity through the transcription factor Spi-B [ Sci Immunol, 2025, 10(109):eads5818] PubMed: 40614214
Nilotinib attenuates vascular pathology in experimental cerebral malaria [ Blood Adv, 2025, bloodadvances.2024015364] PubMed: 39993234
Novel antileukemic compound with sub-micromolar potency against STAT5 addicted myeloid leukemia cells [ Eur J Med Chem, 2025, 284:117211] PubMed: 39746237
Claudin-1 Contributes to Gastrointestinal Stromal Tumors (GIST) Resistance to Imatinib Mesylate (IM) via Regulation of FGFR-Signaling [ Int J Mol Sci, 2025, 26(17)8138] PubMed: 40943068
PBA2, a novel inhibitor of the β-catenin/CBP pathway, eradicates chronic myeloid leukemia including BCR-ABL T315I mutation [ Mol Cancer, 2024, 23(1):209] PubMed: 39342174
Combined targeting of GPX4 and BCR-ABL tyrosine kinase selectively compromises BCR-ABL+ leukemia stem cells [ Mol Cancer, 2024, 23(1):240] PubMed: 39465372
YAP mediates apoptosis through failed integrin adhesion reinforcement [ Cell Rep, 2024, 43(3):113811] PubMed: 38393944
Endothelial HIFα/PDGF-B to smooth muscle Beclin1 signaling sustains pathological muscularization in pulmonary hypertension [ JCI Insight, 2024, 9(10):e162449.] PubMed: 38652543
Cancer-Associated Fibroblasts Promote Lymphatic Metastasis in Cholangiocarcinoma via the PDGF-BB/PDGFR-β Mediated Paracrine Signaling Network [ Aging Dis, 2024, 15(1):369-389] PubMed: 37307823
Cancer-Associated Fibroblasts Promote Lymphatic Metastasis in Cholangiocarcinoma via the PDGF-BB/PDGFR-β Mediated Paracrine Signaling Network [ Aging Dis, 2024, 15(1):369-389] PubMed: 37307823

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。

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