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Imatinib

产品编号 T6230 CAS 152459-95-5

别名: 伊马替尼, STI571, CGP057148B, ST-1571

Imatinib (STI571) 是一种多靶点受体酪氨酸激酶抑制剂，可选择性抑制 BCR/ABL、v-Abl、PDGFR、c-kit 等激酶活性，具有口服活性。Imatinib 具有抗肿瘤活性，可用于治疗慢性粒细胞白血病。

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Imatinib, CAS 152459-95-5

规格	价格/CNY	货期
100 mg	￥ 289	现货
200 mg	￥ 413	现货
500 mg	￥ 747	现货
1 g	￥ 1,260	现货
5 g	￥ 3,180	现货
1 mL * 10 mM (in DMSO)	￥ 455	现货

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其他形式的 Imatinib:

选择批次

纯度: 100%

纯度: 99.94%

纯度: 99.85%

纯度: 99.51%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	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.
靶点活性	c-Kit:100 nM (cell free), PDGFR:100 nM (cell free)
体外活性	方法：人、小鼠和大鼠的骨肉瘤细胞用 Imatinib (1-40 μM) 处理 72 h，使用 XTT assay 检测细胞活力。结果：Imatinib 以剂量依赖性方式降低了活骨肉瘤细胞的数量，72 h 的 IC50 为：20 μM (MG-63)、11 μM (HOS)、23 μM (MOS-J)、15 μM (POS-1)、9 μM (OSRGA）。[1] 方法：人胃癌细胞 AGS、MKN45 和 SNU638 用 Imatinib (30-100 μM) 处理 48 h，使用 Flow Cytometry 检测细胞凋亡情况。结果：Annexin V/PI-positive 细胞的百分比显著增加，表明 Imatinib 治疗增加了肿瘤细胞的早期凋亡。[2]
体内活性	方法：为研究抗肿瘤活性，将 Imatinib (25-100 mg/kg) 口服给药给携带未分化 POS-1 或混合成骨细胞/溶骨 MOS-J 骨肉瘤肿瘤的小鼠，每天一次，持续 21 或 43 天。结果：Imatinib 在体内抑制骨肉瘤的进展。[1] 方法：为研究对多发性硬化症 (MS) 的作用，将 Imatinib (60 mg/kg) 口服给药给 EAE C57BL/6 小鼠模型，每周六次，持续两周。结果：Imatinib 通过减轻疾病的严重程度和延迟发病，对 EAE 有有益的影响。Imatinib 及其潜在的治疗作用和免疫调节特性可被考虑用于治疗多发性硬化症。[3]
细胞实验	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].
动物实验	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].

别名	伊马替尼, STI571, CGP057148B, ST-1571
分子量	493.6
分子式	C29H31N7O
CAS No.	152459-95-5

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 25 mg/mL (50.65 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0259 mL	10.1297 mL	20.2593 mL	50.6483 mL
	5 mM	0.4052 mL	2.0259 mL	4.0519 mL	10.1297 mL
	10 mM	0.2026 mL	1.013 mL	2.0259 mL	5.0648 mL
	20 mM	0.1013 mL	0.5065 mL	1.013 mL	2.5324 mL
	50 mM	0.0405 mL	0.2026 mL	0.4052 mL	1.013 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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.

文献引用

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Imatinib 152459-95-5 Angiogenesis Autophagy Cytoskeletal Signaling Microbiology/Virology Tyrosine Kinase/Adaptors SARS-CoV Bcr-Abl PDGFR c-Kit 伊马替尼 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

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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Imatinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords