PP 2 (AG 1879)
(Synonyms: AGL 1879) 目录号 : GC10344
A selective inhibitor of Src tyrosine kinases
Cas No.:172889-27-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human glioblastoma cell line U251 |
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Preparation method |
Soluble in DMSO > 15.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10μmol/L, 4days for cell proliferation assays; 5μmol/L, 1min for fluorescent time-lapse videomicroscopy images |
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Applications |
A decreased proliferation appeared in the glioma cell cultures treated with 10μmol/L PP2, suggesting thatinhibition of Src family kinase activity in glioma cells resulted in an exit from the cell cycle in monolayers. PP2 caused the disappearance of peripheral membrane ruffles within minutes. |
| Animal experiment [2]: | |
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Animal models |
Female Sprague-Dawley rats |
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Dosage form |
50 μM, 10 μl, intrathecal injection |
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Application |
Pretreatment with PP2 exhibited no effects on the TS(test stimulation)-evoked baseline reflex activity, it prevented ephrinB2-dependent reflex potentiation by decreasing the mean spike count evoked by the TS. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Angers-Loustau A1, Hering R, et al, SRC regulates actin dynamics and invasion of malignant glial cells in three dimensions. Mol Cancer Res, 2004. 2(11): p. 595-605. [2]. Wu HC1, Chang CH, et al, EphrinB2 induces pelvic-urethra reflex potentiation via Src kinase-dependent tyrosine phosphorylation of NR2B. Am J Physiol Renal Physiol, 2011. 300(2): p. F403-11. | |
PP2 is a selective inhibitor of Src family with IC50 value of 4 nM and 5 nM for Lck and Fyn, respectively [1].
Src is a tyrosine kinase and contains 9 members: c-Src (this protein), Yes, Fyn, Fgr, Yrk, Lyn, Blk, Hck, and Lck [1].
PP2 is a potent Src family inhibitor that plays an important role in the cancer and is regarded as a promising target for treatment. When tested with human glioma cell line U251 spheroids in 3-D model, PP2 inhibited the cell invasion in a dose-dependent manner (2.5 μM, 10μM). And treated monolayer U251 cells with PP2 (10μM) decreased cell proliferation rate by inhibiting Src [2]. In human T cells, PP2 showed inhibition on anti-CD3-induced tyrosine phosphorylation by inhibiting Lck and Fyn that involved in the early T cell signal transduction [1].
In Sprague-Dawley rat model injected with urethane and after some needed treatment to perform research and record data, pretreatment with PP2 (50M, 10μL it) reversed the reflex potentiation, as well as Src kinase and NR2B phosphorylation by inhibiting Src family [3].
It is also reported that PP2 inhibits ZAP-70, JAK2 and EGF-R with IC50 value of >100 μM, >50 μM, and 480 nM, respectively [1].
References:
[1]. Hanke, J.H., et al., Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem, 1996. 271(2): p. 695-701.
[2]. Angers-Loustau, A., et al., SRC regulates actin dynamics and invasion of malignant glial cells in three dimensions. Mol Cancer Res, 2004. 2(11): p. 595-605.
[3]. Wu, H.C., et al., EphrinB2 induces pelvic-urethra reflex potentiation via Src kinase-dependent tyrosine phosphorylation of NR2B. Am J Physiol Renal Physiol, 2011. 300(2): p. F403-11.
| Cas No. | 172889-27-9 | SDF | |
| 别名 | AGL 1879 | ||
| 化学名 | 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine | ||
| Canonical SMILES | CC(C)(C)N1C2=C(C(=N1)C3=CC=C(C=C3)Cl)C(=NC=N2)N | ||
| 分子式 | C15H16ClN5 | 分子量 | 301.78 |
| 溶解度 | ≥ 15.1mg/mL in DMSO, ≥ 20.05 mg/mL in EtOH with ultrasonic | 储存条件 | Desiccate at 4°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3137 mL | 16.5684 mL | 33.1367 mL |
| 5 mM | 0.6627 mL | 3.3137 mL | 6.6273 mL |
| 10 mM | 0.3314 mL | 1.6568 mL | 3.3137 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。