Imatinib Mesylate (STI571)

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

Imatinib Mesylate (STI571)化学構造


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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  • 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.

    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.

  • 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.

    (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.
(Cell-free assay)
c-Kit [2]
(M-07e cells)
v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM

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]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D  M2jrZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXJeolTUUN3ME21NEDPxE1? MoPJNlU5PjN{M{K=
Hep G2 NX;t[mR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnpTWM2OD1|MTFOwG0> NGjBV|YzPTh4M{KzNi=>
DU145 NH;oPIZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUOyNQKBkc7:TR?= MWS2MVczKGh? M4q5bYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= NIfVRXozPTd6Nk[1Oi=>
PC3  NVzicoJLS2WubDDWbYFjcWyrdImgRZN{[Xl? MknXNlDjiIoQvF2= MlLhOk04OiCq MVrpcoNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? MlToNlU4QDZ4NU[=
DU145 MXHBdI9xfG:|aYOgRZN{[Xl? NILKRnAzOOLCid88US=> NYfRNo5NPDhxN{KgbC=> NGXIb3FqdmS3Y3XzJINmdGxiZHXheIgh[nliYYDvdJRwe2m| MmPnNlU4QDZ4NU[=
PC3  MV3BdI9xfG:|aYOgRZN{[Xl? M4fueFIx6oDLzszN M2XvN|Q5Nzd{IHi= NE\ISoRqdmO{ZXHz[ZMh[2WubDDzeZJ3cX[jbB?= NY\ZS3NMOjV5OE[2OVY>
MCF-7 M3HB[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DRR|ExKM7:TR?= M3nTV|Q5KGh? MofPZoxw[2u|IHPlcIwheHKxbHnm[ZJifGmxbjDpcoNz\WG|ZTDpcoR2[2WmIHL5JGJLO1p? NHTKTmEzPTJ5NECzOC=>
K-562  MojaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XuSWlEPTB;MTFOwG0> MnHXNlUzOzl4NkK=
K562  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwNdMg{txO Mm\1NlQ6Ozl2MUi=
K562r NVXTNmZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGO4OoRKSzVyPUGwxsDPxE1? MkW0NlQ6Ozl2MUi=
K562 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr6cWJGSzVyPUCuNFkh|ryP MoniNVY3Pzh2MUS=
K562 MX\DfZRwfG:6aXPpeJkhSXO|YYm= NVLydIt7OjRiaB?= M2PPOmlEPTB;MD6yNUDPxE1? M3rFS|IzODByMkC3
MDA-MB-23 M3ruNmN6fG:2b4jpZ4l1gSCDc4PhfS=> MknQNlQhcA>? MYPJR|UxRTFwODFOwG0> M1TlRlIzODByMkC3
GIST882 M3;N[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jKRVk3KGh? M1nWdWlEPTB;MT63JO69VQ>? MYqyOFkxODJzMh?=


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]


+ 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.
+ 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.

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):
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。


分子量 589.71


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





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


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

  • C1



  • 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):




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


質量 濃度 体積 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03674099 Recruiting Multiple Sclerosis Tomas Olsson|The Swedish Research Council|Karolinska Institutet October 1 2018 Phase 2
NCT03688568 Recruiting Neurofibroma Plexiform Indiana University|Food and Drug Administration (FDA) September 1 2018 Phase 2
NCT03516279 Not yet recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Minimal Residual Disease ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group August 12 2018 Phase 2
NCT02538926 Withdrawn 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) July 1 2018 Phase 2
NCT03131999 Recruiting Lymphangioleiomyomatosis Medical University of South Carolina|Columbia University January 23 2018 Phase 1|Phase 2
NCT03241199 Recruiting Chronic Myeloid Leukemia|Philadelphia Chromosome Positive CML The University of Hong Kong August 1 2017 Phase 2



Handling Instructions


  • * 必須


Bcr-Abl Inhibitors with Unique Features


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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