| 中文名称: | PP2 | ||||
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| 英文名称: | PP2 | ||||
| 别名: | PP2 AG1879；1-(tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine | ||||
| CAS No: | 172889-27-9 | 分子式: | C15H16ClN5 | 分子量: | 301.77 |
| CAS No: | 172889-27-9 | ||||
| 分子式: | C15H16ClN5 | ||||
| 分子量: | 301.77 | ||||
基本信息
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产品编号：P10520 |
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产品名称：PP2 |
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CAS: |
172889-27-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
301.77 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
60mg/mL (198.82mM) |
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Ethanol |
2mg/mL (6.62mM) |
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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 |
3.3138mL |
16.5689mL |
33.1378mL |
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5mM |
0.6628mL |
3.3138mL |
6.6276mL |
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10mM |
0.3314mL |
1.6569mL |
3.3138mL |
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50mM |
0.0663mL |
0.3314mL |
0.6628mL |
生物活性
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产品描述 |
一种可逆的ATP竞争性的Src家族抑制剂，抑制Lck和Fyn。 |
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靶点/IC50 |
IC50: 4nM (Lck), 5nM (Fyn) |
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体外研究 |
At 10μM, the effect of PP2 on cellular proliferation is not significant, indicating that, at this low concentration, the effect of PP2 on Gemcitabine cytotoxicity does not simply reflect a direct antiproliferative effect, but rather a potentiation of Gemcitabine-induced cytotoxicity. Above 20μM, growth is increasingly suppressed, a finding consistent with reports in other human cancer cell lines. Although 10μM PP2 is used in our study, at higher concentrations PP2 is reported to inhibit other intracellular kinases. PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50 of ~5nM in vitro, concentrations to 10μM are often necessary to achieve complete Src family kinase inhibition in cell culture. |
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体内研究 |
The tumor growth inhibition rate is 25% in the PP2 treatment group and 5% in the Gemcitabine treatment group (P>0.05). When administered in combination, PP2 and Gemcitabine produce a tumor growth inhibition rate of 98% (P<0.05). Hepatic metastasis occurred in 100% of control and Gemcitabine-treated groups; 88% of the PP2-treated group developed liver metastases. There are no detectable metastases in the group treated with PP2 and Gemcitabine in combination (P<0.05). |
推荐实验方法(仅供参考)
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细胞实验: |
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Cell growth is determined by MTT assay and confirmed by cell counting. Results of the MTT assay have been shown to correlate well with [3H]thymidine incorporation in pancreatic cancer cell lines.Logarithmically growing cells are plated at 5×103 cells/well in 96-well plates, allowed to adhere for 24h, and cultured in the presence or absence of PP2 and Gemcitabine. Cell proliferation is determined after 96h.Plates are read using a Vmax microplate spectrophotometer at a wavelength of 570nm corrected to 650 nm and normalized to controls. Each independent experiment is performed three times, with 10 determinations for each condition tested. The IC50 of Gemcitabine is calculated from these results. At identical time points, cells are trypsinized to form a single cell suspension. Intact cells, determined by trypan blue exclusion, are counted using a Neubauer hemocytometer, and the number of cells per mL is calculated and compared with the control group to confirm the MTT results. |
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动物实验: |
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Mice Male athymic nu/nu mice (age, 5 weeks; weight, 20-22g; specific pathogen free) are anesthetized with i.p.ketamine (200mg/kg) and xylazine (10mg/kg) and inoculated with 106 Gemcitabine-resistant PANC1GemRes cells in 20μL of PBS by surgical orthotopic implantation into the pancreas. After inoculation, mice are randomized to three treatment groups:(a) treatment group 1(n=8) receive 2 mg/kg PP2 in 1% DMSO by i.p.injection three times a week;(b) treatment group 2(n=8) receive Gemcitabine (100mg/kg) in the same volume of 1% DMSO vehicle as received by group 1, three times a week; and (c) treatment group 3 (n=8) receive 2mg/kg PP2 and 100mg/kg Gemcitabine in the same volume of DMSO as groups 1 and 2, three times a week. The control group receive the same volume of 1% DMSO vehicle as the other groups, three times a week. Treatment is commenced 1 day after implantation, and necropsy is performed 4 weeks after implantation. Primary tumors are identified, weighed, and normalized to total body mass. Tumor growth inhibition rate is calculated using the following formula: tumor growth inhibition rate (%)=(1−MT/MC)×100, where MT and MC are the mean normalized tumor masses of treatment and controlgroups,respectively. Liver metastases are counted and confirmed histologically. |
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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 )
