| 中文名称: | 埃罗替尼甲磺酸盐 | ||||
|---|---|---|---|---|---|
| 英文名称: | Erlotinib mesylate | ||||
| 别名: | 甲磺酸厄洛替尼;厄洛替尼甲磺酸盐 CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylate | ||||
| CAS No: | 248594-19-6 | 分子式: | C23H27N3O7S | 分子量: | 489.54 |
| CAS No: | 248594-19-6 | ||||
| 分子式: | C23H27N3O7S | ||||
| 分子量: | 489.54 | ||||
基本信息
|
产品编号：E10382 |
|||||
|
产品名称：Erlotinib mesylate |
|||||
|
CAS: |
248594-19-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
分子式： |
|||||
|
分子量 |
489.54 |
||||
|
化学名： |
|
||||
|
Solubility (25°C) |
体外 |
DMSO |
|
||
|
Ethanol |
|
||||
|
Water |
|
||||
|
体内 |
现配现用 |
|
|||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
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。 |
|||||
|
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。 |
|||||
生物活性
|
产品描述 |
为 EGFR 抑制剂，IC50 值为 2nM。 |
|
靶点/IC50 |
EGFR 2nM (IC50) |
|
体外研究 |
Erlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50 of 1nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50 of 100nM for an 8-day proliferation assay. The combination of B-DIM and Erlotinib (2μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone. |
|
体内研究 |
There is a 1.49-fold statistically significant difference between AUC0-inf after p.o. administration of Erlotinib (5mg/kg) comparing Bcrp1/Mdr1a/1b-/- and WT mice (7,419±1,720 versus 4,957±1,735ng*h/mL respectively, P=0.01). The administration of Erlotinib (10 mg/kg/day, or 20mg/kg/day) to Bleomycin (BLM)-treated rats shows no exacerbation of lung injuries in indices such as macroscopic findings, lung weights, histopathological scores (lung lesion density and lung fibrosis score), and pulmonary hydroxyproline (HyP) level. The result suggests that Erlotinib does not have any exacerbating effects on lung injuries induced by BLM in rats. |
推荐实验方法(仅供参考)
|
激酶实验： |
|
The kinase reaction is performed in 50μL of 50mM HEPES (pH 7.3), containing 125mM NaCl, 24mM MgCl2, 0.1 mM Na3VO4,20μM ATP, 1.6μg/mL EGF, and 15ng of EGFR, affinity purified from A431 cell membranes. The compound in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8mm at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with wash buffer. Phosphorylated PGT is measured by 25mim of incubation with 50μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with wash buffer. The colonmetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09M sulfuric acid, 50μL per well.Phosphotyrosine is estimated by measurement of absorbance at 450nm. The signal for controls is typically 0.6-1.2absorbance units, with essentially no back ground in wells without AlP, EGFR, or POT and is proportional to the time of incubation for 10mm |
|
细胞实验: |
|
|
To test the viability of cells treated with B-DIM, Erlotinib, or the combination, BxPC-3 and MIAPaCa cells are plated (3,000-5,000 per well) in a 96-well plate and incubated overnight at 37°C. A range of concentrations for both B-DIM (10-50µM) and Erlotinib (1-5µM) is initially tested. Based on the initial results, the concentration of B-DIM (20µM) and Erlotinib (2µM) are chosen for all assays. The effects of B-DIM (20 µM), Erlotinib (2µM), and the combination on BxPC-3 and MIAPaCa cells are determined by the standard MTT assay after 72h and is repeated three times. The color intensity is measured by a Tecan microplate fluorometer at 595nm. DMSO treated cells are considered to be the untreated control and assigned a value of 100%. In addition to the above assay, we have also done clonogenic assay for assessing the effects of treatment. |
|
|
动物实验: |
|
|
and WT mice are treated p.o. or i.p. with 5mg/kg Erlotinib. The i.p. administration is chosen assuming good drug absorption and complete bioavailability. Sampling is done from the tip of the lateral tail vein in three series.During the first series, whole blood samples are collected at 15min and 0.5, 1.5, 5, and 10h after injection. Based on the results of this initial group, the sampling times of the two subsequent series are adapted to 5 and 15min and 0.5, 1.5, 4, and 8h after injection. After collection, the blood samples are immediately centrifuged and plasma is stored at -20°C until highperformance liquid chromatographic analysis took place.Rats Seven-week-old male Crl:CD (SD) rats (244-297 g) are used. The animals are treated with Erlotinib (10mg/kg and 20mg/kg)orally by gavage.
|
|
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 )
