产品说明书
PD0166285
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同义名 : | - |
| CAS号 : | 185039-89-8 | |
| 货号 : | A795383 | |
| 分子式 : | C26H27Cl2N5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 512.431 | |
| MDL号 : | MFCD00950060 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(97.57 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Wee1 is a tyrosine kinase belonging to the Ser/Thr family of protein kinases. Wee1 catalyzes the inhibitory tyrosine phosphorylation of CDC2/cyclin B kinase, and appears to coordinate the transition between DNA replication and mitosis by protecting the nucleus from cytoplasmically activated CDC2 kinase. In details, wee1 acts as a negative regulator of mitosis (G2 to M transition) by protecting the nucleus from cytoplasmically activated cyclin B1-complexed CDK1 before the onset of mitosis by mediating phosphorylation of CDK1 on Tyr-15[3]. PD0166285 is a wee1 inhibitor. Data obtained by a wee1 mass screening revealed that the inhibitory IC50 of PD0166285 against wee1 was 24 nM[2]. PD0166285 also inhibited myt1 kinase, a dual-specificity protein kinase that phosphorylates Cdc2 on both Thr 14 and Tyr 15[4] with an IC50 of 72 nM[2]. 0.5μM PD0166285 dramatically inhibited irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in the cancer cell lines of hct116, HT29, DLD-1, hct8, H460, Hela and C26[2]. In a cell cycle assay, G2 arrest in HT29 cells were induced by irradiation as evidenced by the increase of G2-M population to 66-69%. 4h treatment of PD0166285 at the concentration of 0.25 μM decreased the G2-M cell population to 37%[2]. According to another report, 4h treatment of 0.5 μM PD0166285 resulted in decrease of cyclin D mRNA to 42.1% of baseline level as revealed by real-time PCR in B16 cells[1]. In an E98 orthotopic tumor model established by intracranial injection of tumor cells into Balb/c nude mice, PD0166285 was administrated daily at the concentration of 20 μM via i.p. injection for 5 days. The results was that PD0166285 improved survival of tumor bearing mice[5]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| C6 cell | Function assay | Inhibition of C6 cell proliferation in sulforhodamine B assay, IC50=0.34 μM | 9703473 | ||
| C6 cells | Function assay | Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells, IC50=5 nM | 9703473 | ||
| HCT-8 | Function assay | Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined, IC50=0.42 μM | 10956222 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.20mL |
9.76mL 1.95mL 0.98mL |
19.51mL 3.90mL 1.95mL |
| 参考文献 |
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