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CAS No.: 185039-89-8

PD0166285 Catalog No. CSN19234

Synonyms: PD0166285

PD0166285 inhibits Wee1 and Chk1 at nanomolar concentrations and can hinder G2 checkpoint.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9515 mL
- 9.7574 mL
- 19.5148 mL
- 5 mM
- 0.3903 mL
- 1.9515 mL
- 3.9030 mL
- 10 mM
- 0.1951 mL
- 0.9757 mL
- 1.9515 mL

技术信息

CAS号

185039-89-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H27Cl2N5O2

运输

蓝冰

分子量

512.43

别名

PD0166285

溶解度

DMSO	30.0 mg/mL (58.5 mM)
Water	insoluble

动物实验配方

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