| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408365-1ml |
1ml |
现货  |
|
| 英文别名 | AG 1879,AGL 1879 | 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(4-chlorophenyl)-1-(1,1-dimethylethyl)- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PP2 |
| 生化机理 | PP2（AG 1879，AGL 1879）是一种 Src 家族激酶抑制剂，对 Lck/Fyn 有很强的抑制作用，在无细胞实验中的 IC50 为 4 nM/5 nM，对表皮生长因子受体的抑制作用要低约 100 倍，对 ZAP-70、JAK2 和 PKA 没有活性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | FYN 原癌基因抑制剂; Src 家族酪氨酸激酶; LCK 原癌基因抑制剂; Src 家族酪氨酸激酶 |
| 产品介绍 |
PP2(AGL 1879) 是可逆的ATP竞争性的Src家族抑制剂，对p56lck，p59fynT，Hck和Src的IC50分别为4，5，5和100 nM。An effective and selective inhibitor of Src family kinases Information PP2 PP2 (AG 1879, AGL 1879), a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA. PP2 inhibits Src by binding to an area of the molecule that does not overlap with the ATP binding domain. PP2 (20 μM) induces 40-50% growth inhibition of HT29 cells, this concentration reduces the Src activity as early as 1 hour and maintains a 35% inhibition of Src activity for 2 days. PP2 (100 mM) decreases the Src activity of HT29 cells in a dose-dependent manner. PP2 (1 mM-100 mM) causes a dose-dependent growth inhibition of human colon cancer cells (HT29, SW480, and PMCO1), liver cancer cells (PLC/PRF/5, KYN-2, Li7, and HepG2), and breast cancer cells (MCF-7, MDA-MB-468, and BT-474). PP2 (20 μM) significantly increases aggregation in most of the cancer cells (HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, MCF-7, and MDA-MB-468) in E-cadherin dependent manner. PP2 (20 μM) enhances E-cadherin expression and also strongly increases E-cadherin’s association with the actin cytoskeleton in cancer cells. PP2 (20 μM) increases the expression of α-catenin, β-catenin, and γ-catenin in HT29 cells, whereas in PLC/PRF/5 and MCF-7 cells, the total protein level of α-catenin does not change, but the levels of β- catenin and γ-catenin increases slightly. PP2 inhibits proliferation of two cervical cancer cells (HeLa and SiHa) in a time- and dose-dependent manner. PP2 (10 μM) down-regulates pSrc-Y416, pEGFR-Y845, and -Y1173 expression levels in HeLa and SiHa cells. PP2 (10 μM) could modulate cell cycle arrest by up-regulating p21(Cip1) and p27(Kip1) in both HeLa and SiHa cells and down-regulating expression of cyclin A, and cyclin dependent kinase-2, -4 (Cdk-2, -4) in HeLa and of cyclin B and Cdk-2 in SiHa. In vivo PP2 (5 mg/kg/day) induces some slowing in the growth rate of the primary tumors relative to the control treated with vehicle in SCID mice inoculated HT29 cells in the spleen. PP2 (5 mg/kg/day) induces some slowing in the growth rate of the primary tumors relative to the control treated with vehicle in SCID mice inoculated HT29 cells in the spleen. PP2 (5 mg/kg/day) significantly reduces the relative liver weight and liver metastasis volume compared with the controls in SCID mice inoculated HT29 cells in the spleen. PP2 (1.5 mg/kg i.p.) treated rats show approximately 50% reduction of infarct size on T2-weighted MRI and in TTC staining compared with controls in rats with focal ischemic brain injury. PP2 (1.5 mg/kg i.p.) results in better the neurological score than controls in rats with focal ischemic brain injury. cell lines：CEM/VLB100, P388/ADR, MCF7/ADR, 2780AD, and UCLA-P3.OO3VLB cells Concentrations：~100 μM Incubation Time：2 days Powder Purity:≥99% |
| EC号 | 878-892-3 |
|---|---|
| 分子类型 | 小分子 |
| Isomeric SMILES | CC(C)(C)N1C2=NC=NC(=C2C(=N1)C3=CC=C(C=C3)Cl)N |
| 关联CAS | 172889-27-9 |
| MeSH Entry Terms | 4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo(3,4-d)pyrimidine;AG 1879;AG1879;PP2 cpd;Src family kinase inhibitor PP2 |
| 分子量 | 301.77 |
| Reaxy-Rn | 9409964 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9409964&ln= |
| 折光率 | 1.68 |
|---|---|
| 沸点 | 493.54° C at 760 mmHg |
| 熔点 | 193.32°C |
| 1. Yijun Li, Xinyu Wen, Min Nie, Qi Wang. (2017) Toward Subtle Manipulation of Fine Dendritic β-Nucleating Agent in Polypropylene. ACS Omega, 2 (10): (7230–7238). [PMID:31457299] [10.1021/acsomega.7b01036] |
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