Imatinib

カタログ番号 T6230 CAS 152459-95-5

別名: STI571, CGP057148B, ST-1571

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

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Imatinib, CAS 152459-95-5

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
100 mg	在庫あり	￥ 8,500
200 mg	在庫あり	￥ 12,000
500 mg	在庫あり	￥ 18,500
1 g	在庫あり	￥ 27,000
5 g	在庫あり	￥ 48,000
1 mL * 10 mM (in DMSO)	在庫あり	￥ 13,000

バルクのお問い合わせ

バッチを選択

純度: 100%

COA DATASHEET SDS HNMR HPLC

純度: 99.94%

COA DATASHEET SDS HPLC HNMR

純度: 99.85%

COA DATASHEET SDS HPLC HNMR

純度: 99.51%

COA DATASHEET SDS HNMR HPLC

COA DATASHEET SDS

DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.
ターゲット＆IC50	c-Kit:100 nM (cell free), PDGFR:100 nM (cell free)
In vitro	METHODS: Human, mouse and rat osteosarcoma cells were treated with Imatinib (1-40 μM) for 72 h, and cell viability was measured using XTT assay. RESULTS: Imatinib reduced the number of live osteosarcoma cells in a dose-dependent manner, with 72 h IC50s of 20 μM (MG-63), 11 μM (HOS), 23 μM (MOS-J), 15 μM (POS-1), and 9 μM (OSRGA). [1] METHODS: Human gastric cancer cells AGS, MKN45 and SNU638 were treated with Imatinib (30-100 μM) for 48 h. Apoptosis was detected using Flow Cytometry. RESULTS: The percentage of Annexin V/PI-positive cells was significantly increased, indicating that Imatinib treatment increased early apoptosis of tumor cells. [2]
In vivo	METHODS: To investigate antitumor activity, Imatinib (25-100 mg/kg) was administered orally to mice bearing undifferentiated POS-1 or mixed osteoblast/osteolytic MOS-J osteosarcoma tumors once daily for 21 or 43 days. RESULTS: Imatinib inhibited osteosarcoma progression in vivo. [1] METHODS: To study the effects on multiple sclerosis (MS), Imatinib (60 mg/kg) was administered orally six times per week for two weeks to an EAE C57BL/6 mouse model. RESULTS: Imatinib had beneficial effects on EAE by reducing disease severity and delaying onset.Imatinib and its potential therapeutic effects and immunomodulatory properties may be considered for the treatment of multiple sclerosis. [3]
細胞研究	M-07e cells were grown in serum-free RPMI 1640 at 37°C for approximately 18 hours before they were incubated for 90 minutes in the presence of various concentrations of STI 571. The cells were then pelleted and resuspended in 1 mL RPMI 1640. STI 571 was added to each tube to achieve the same concentration used during the 90 minutes of preincubation. The cells were then incubated with inhibitor and growth factor (SLF or GM-CSF) for 15 minutes at 37°C. Subsequently, the cell pellets were lysed with 100 to 250 μL of protein lysis buffer (50 mmol/L Tris, 150 mmol/L sodium chloride, 1% NP-40, and 0.25% deoxycholate, with addition of the inhibitors aprotinin, leupeptin, pepstatin, phenylmethyl sulfonyl fluoride, and sodium orthovanadate). Western immunoblot analysis was performed as previously described.41Experiments with HMC-1 cells were performed in the same way except that neither SLF nor GM-CSF was added [1].
動物実験	Swiss mice (nu/nu, female), weighing 30 g, 6 – 8 weeks old, were bred in the animal facilities, maintained under specific pathogen-free conditions with artificial lighting (12 hr light/12 hr dark cycle) and fed a regular diet and water ad libitum. For therapeutic trials, the tumor-bearing mice were randomly divided into equivalent groups of 5 to 12 animals and mice were treated as soon as the xenografted tumors reached a diameter of 5 mm (or a tumor volume of approximately 60 mm^3). Four different human tumors were used: the SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers. STI571 was administered at a total dosage of 70 or 100 mg/kg per day in 1 or 2 intraperitoneal injections, with or without etoposide plus ifosfamide or topotecan. STI571 was diluted in 150 l of H2O and administered on different days, as indicated. Etoposide and ifosfamide were diluted in 200 l of 0.9% sodium chloride, and topotecan was diluted in 150 l of 0.9% sodium chloride. The control group received injections according to the same schedule as experimentally treated mice. All mice were weighed once weekly. Tumor growth was monitored by measuring 2 perpendicular diameters with calipers. Tumor volume (V) and the relative tumor volume (RTV) were calculated as:. V = a^2 × b/2,. where a is the width (large diameter) and b the length (small. diameter) of the tumor in millimeters, and. RTV = Vx/Vi,. where Vx is the mean tumor volume in cubic millimeters at any given time and Vi is the mean initial tumor volume in cubic millimeters at the start of treatment. Mice were ethically sacrificed when the tumor volume reached 2,500 mm^3 [5].

別名	STI571, CGP057148B, ST-1571
分子量	493.6
分子式	C29H31N7O
CAS No.	152459-95-5

保存条件

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 25 mg/mL (50.65 mM)

参考文献

1. Gobin B, et al. Imatinib mesylate exerts anti-proliferative effects on osteosarcoma cells and inhibits the tumour growth in immunocompetent murine models. PLoS One. 2014 Mar 5;9(3):e90795. 2. Kim JL, et al. Imatinib‑induced apoptosis of gastric cancer cells is mediated by endoplasmic reticulum stress. Oncol Rep. 2019 Mar;41(3):1616-1626. 3. Azizi G, et al. Effects of imatinib mesylate in mouse models of multiple sclerosis and in vitro determinants. Iran J Allergy Asthma Immunol. 2014 Jun;13(3):198-206. 4. Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63. 5. Decaudin D, et al. In vivo efficacy of STI571 in xenografted human small cell lung cancer alone or combined with chemotherapy. Int J Cancer. 2005 Feb 20;113(5):849-56. 6. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 7. Liu H M, Guo C L, Zhang Y F, et al. Leonurine-repressed miR-18a-5p/SOCS5/JAK2/STAT3 axis activity disrupts CML malignancy[J]. Frontiers in Pharmacology. 2021, 12.

引用文献

1. Wang B, He B S, Ruan X L, et al. An integrated microfluidics platform with high-throughput single-cell cloning array and concentration gradient generator for efficient cancer drug effect screening. Military Medical Research. 2022, 9(1): 1-17. 2. Li Q, Huang Z, Peng Y, et al. RanBP3 Regulates Proliferation, Apoptosis and Chemosensitivity of Chronic Myeloid Leukemia Cells via Mediating SMAD2/3 and ERK1/2 Nuclear Transport. Frontiers in Oncology. 2021: 3349. 3. Zhou D, Yang S, Yan H, et al. SC75741, a novel c-Abl inhibitor, promotes the clearance of TDP25 aggregates via ATG5-dependent autophagy pathway. Frontiers in Pharmacology. 2021: 2891. 4. Zeng D, Gao M, Zheng R, et al. The HSP90 inhibitor KW-2478 depletes the malignancy of BCR/ABL and overcomes the imatinib-resistance caused by BCR/ABL amplification. Experimental Hematology & Oncology. 2022, 11(1): 1-14 5. Zeng D, Gao M, Zheng R, et al. The HSP90 inhibitor KW-2478 depletes the malignancy of BCR/ABL and overcomes the imatinib-resistance caused by BCR/ABL amplifcation. Experimental Hematology & Oncology. 2022, 11(1): 1-14 6. Liu H M, Guo C L, Zhang Y F, et al. Leonurine-repressed miR-18a-5p/SOCS5/JAK2/STAT3 axis activity disrupts CML malignancy. Frontiers in Pharmacology. 2021, 12. 7. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 8. Qin R, Wang T, He W, et al.Jak2/STAT6/c-Myc pathway is vital to the pathogenicity of Philadelphia-positive acute lymphoblastic leukemia caused by P190BCR-ABL.Cell Communication and Signaling.2023, 21(1): 27.

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Imatinib 152459-95-5 Angiogenesis Autophagy Cytoskeletal Signaling Microbiology/Virology Tyrosine Kinase/Adaptors Bcr-Abl PDGFR c-Kit SARS-CoV CGP-57148B Platelet-derived growth factor receptor SCFR STI571 Inhibitor ST 1571 SARS coronavirus STI 571 inhibit CD117 CGP057148B ST1571 STI-571 ST-1571 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Imatinib

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords