| 中文名称: | Imatinib mesylate 促销 | ||||
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| 英文名称: | Imatinib mesylate | ||||
| 别名: | 甲磺酸伊马替尼 CGP57148；N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonate | ||||
| CAS No: | 220127-57-1 | 分子式: | C29H31N7O.CH4O3S | 分子量: | 589.71 |
| CAS No: | 220127-57-1 | ||||
| 分子式: | C29H31N7O.CH4O3S | ||||
| 分子量: | 589.71 | ||||
| EINEC: | 7142 | ||||
| EINEC: | 7142 | ||||
基本信息
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产品编号：I10051 |
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产品名称：Imatinib mesylate |
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CAS: |
220127-57-1 |
储存条件 |
粉末 |
2-8℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
589.71 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
118mg/mL (200.09mM) |
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Ethanol |
118mg/mL (200.09mM) |
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Water |
Insoluble |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.6957mL |
8.4787mL |
16.9575mL |
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5mM |
0.3391mL |
1.6957mL |
3.3915mL |
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10mM |
0.1696mL |
0.8479mL |
1.6957mL |
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50mM |
0.0339mL |
0.1696mL |
0.3391mL |
生物活性
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产品描述 |
一种酪氨酸激酶抑制剂,可抑制c-Kit、Bcr-Abl和PDGFR(IC50:100nM)。 |
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靶点/IC50 |
PDGFR |
c-Kit |
v-Abl |
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100nM |
100nM |
600nM |
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体外研究 |
Imatinib (STI571) Mesylate inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100nM. Imatinib (STI571) mesylate is very effective (in vitro IC50 of 25nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410nM) and PDGFR (in vitro IC50, 380nM)[2]. Imatinib(STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive(Ph+) acute lymphoblastic leukemia (ALL). |
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体内研究 |
Animals treated with Imatinib Mesylate show a decrease of mean body weight throughout the whole study. Body weight loss is noticeable in mice from groups that receive chemotherapy and the vitamin D analog combined treatment. The body weight decrease of mice treat with both combined Imatinib mesylate and PRI-2191 is the highest (15%) on Day 22 of the experiment, but after that day, mice start to recover. In a rat Ischemia/reperfusion injury (IRI) model, Imatinib mesy lateattenuates lung injury by an antipermeability and antiinflammatory effect. The delivery and function of Imatinib mesylate in the lung is also confirmed in this model. |
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推荐实验方法(仅供参考)
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细胞实验: |
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Tested A549 cells are placed in 96-well flat-bottom plates at a density of 5×103 cells per well 24h before the addition of the test compounds. The cells are incubated for 96h with two different concentrations (10 and 100nM) of PRI-2191 and concurrently with various concentrations of Imatinib mesylate (10, 100, 1000 and 10,000ng/mL) and other cytostatic drugs (Docetaxel (DTX) or Idarubicin (ID) : 0.1, 1, 10, 100ng/mL; Cisplatin (CIS): 1, 10, 100, 1000ng/mL). The sulforhodamine B (SRB) assay is performed to evaluate the cytotoxic effect. As a result, IC50 is calculated for each separate experiment in Cheburator 0.4, Dmitry Nevozhay software. |
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动物实验: |
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Mice NOD/SCID female mice, 12-16 weeks old, body weight of 20-25g, are used. Mice are subcutaneously (s.c.) inoculated in the right flank of the abdomen with A549 tumor cells suspension (5×106 cells in 0.2mL of Hank’s medium per mouse, Day 0) and then are randomized into groups receiving varied combinations of vitamin D analogs and chemotherapeutics. One out of two experimental protocols is applied in the respective experiments: 1. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 75mg/kg/day, daily for 19 days (from Days 7-25). PRI-2191 is administered s.c. or by oral gavage at a dose of 2μg/kg/day, 3 times a week (on Days 7, 12, 14, 16, 19, 21 and 23). 2. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 50 mg/kg/day, daily for 13 days (from Days 7-19). PRI-2191 and PRI-2205 are administered s.c. at doses of 1 or 10g/kg/day,respectively, 3 times a week (on Days 7, 10, 12, 14, 17, 19, 21, 24 and 26). At the end of the experiments, blood is collected under anesthesia; then,the mice are sacrificed. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
