Name: Imatinib Mesylate
Brand: TargetMol
SKU: T1621
Price: 298 CNY
Availability: InStock
Rating: 5 (10 reviews)

Imatinib Mesylate

很棒

产品编号 T1621Cas号 220127-57-1

别名 甲磺酸伊马替尼, STI-571, ST-1571 Mesylate, CGP-57148B

Imatinib Mesylate (STI571 Mesylate) 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 Mesylate 具有抗肿瘤活性，可用于治疗慢性粒细胞白血病。

规格

价格

库存

数量

100 mg

¥ 298

In stock

200 mg

¥ 417

In stock

500 mg

¥ 756

In stock

5 g

¥ 3,930

In stock

1 mL x 10 mM (in DMSO)

¥ 387

In stock

产品介绍

生物活性

产品描述	Imatinib Mesylate (STI571 Mesylate) 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 Mesylate has antitumor activity for the treatment of chronic granulocytic leukemia.
靶点活性	PDGFR:0.3 μM, c-Kit:0.1 μM, MG-63 cells:20 µM, HOS cells:11 µM, OSRGA cells:9 μM, POS-1 cells:15 µM, Vero C1008 cells:3.24 μM, MOS-J cells:23 µM, SGC-7901 cells:0.208 μM
体外活性	方法：人、小鼠和大鼠的骨肉瘤细胞用 Imatinib Mesylate (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 Mesylate (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 Mesylate (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 Mesylate (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	Cells were added to 96-well plates at a density of 20?000 cells/well for HMC-1 and 50?000 cells/well for M-07e. Experiments with M-07e were performed with the use of GM-CSF or SLF as a growth factor supplement. Experiments using HMC-1 were performed without growth factor supplementation. Proliferation at 48 hours was measured with an XTT-based assay [1].
动物实验	Heterozygous experimental TRAMP mice were obtained by breeding wild-type C57BL/6 male mice and heterozygous female TRAMP mice. MC-deficient C57BL/6-KitW-sh/W-sh mice were intercrossed over 12 generations with TRAMP mice to obtain MC-deficient KitWsh-TRAMP mice. Cromolyn (10 mg/kg dissolved in saline; Sigma Aldrich) or imatinib (50 mg/kg dissolved in saline) were administered intraperitoneally in TRAMP mice for 5 days/week. Treatments started at 8 or 16 weeks, as indicated in text and figures, and continued for the duration of the experiment. Mice were sacrificed at 25 weeks and their urogenital apparatus collected for IHC [4].
别名	甲磺酸伊马替尼, STI-571, ST-1571 Mesylate, CGP-57148B

化学信息

分子量	589.71
分子式	C₂₉H₃₁N₇O·CH₄SO₃
CAS No.	220127-57-1
Smiles	CS(O)(=O)=O.CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
密度	0.858 g/mL at 25 °C(lit.)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: 59 mg/mL (100.05 mM), Sonication is recommended.

DMSO: 237.5 mg/mL (402.74 mM), Sonication is recommended.

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6957 mL	8.4787 mL	16.9575 mL	84.7874 mL
5 mM	0.3391 mL	1.6957 mL	3.3915 mL	16.9575 mL
10 mM	0.1696 mL	0.8479 mL	1.6957 mL	8.4787 mL
20 mM	0.0848 mL	0.4239 mL	0.8479 mL	4.2394 mL
50 mM	0.0339 mL	0.1696 mL	0.3391 mL	1.6957 mL
100 mM	0.0170 mL	0.0848 mL	0.1696 mL	0.8479 mL

体内实验配液计算器