中文名称: PF-670462
英文名称: PF-670462
CAS No: 950912-80-8
分子式: C19H20FN5.2HCl
分子量: 410.32
P10883 PF-670462 ≥98% (psaitong)
包装规格:
5g 10mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(≥ 32 mg/mL)
产品描述:

基本信息

产品编号:P10883

产品名称:PF-670462

CAS:

950912-80-8

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C19H20FN5.2HCl

溶于液体

-80℃

两年

分子量

410.32

-20℃

一个月

化学名: 

4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine Dihydrochloride

 

Solubility (25°C)

 

体外

DMSO

82mg/mL (199.84mM)

Ethanol

25mg/mL (60.92mM)

Water

82mg/mL (199.84mM)

体内

现配现用

 

1mg/ml表示微溶或不溶。

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。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.4371mL

12.1856mL

24.3712mL

5mM

0.4874mL

2.4371mL

4.8742mL

10mM

0.2437mL

1.2186mL

2.4371mL

50mM

0.0487mL

0.2437mL

0.4874mL

 

生物活性

产品描述

一种有效的,选择性的 casein kinase (CKIε/CKIδ) 抑制剂,IC50 值分别为 7.7nM 和 14nM。

靶点/IC50

CK1δ 
(Cell-free assay)

13nM

CK1ε 
(Cell-free assay)

90nM

 

体外研究

PF-670462 is a potent and selective inhibitor of CKIε and CKIδ, with IC50s of 7.7nM and 14nM, respectively. PF-670462 shows less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC50s of 150nM and 190nM, respectively. PF-670462 also causes a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC50 of 290 ± 39nM in CKI

ε-transfected COS7 cells. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC50 of -17nM. PF-670462 (1μM) is a weak inhibitor of proliferation, and only modestly suppresses the growth of HEK293 and HT1080 cells. PF-670462 (100nM) strongly inhibits CK1ε and CK1δ, consistent with its effect on Wnt/β-catenin signaling.

 

体内研究

PF-670462 (50mg/kg, s.c.) produces robust phase delays, and the activity remains persistent, with no discernible correction in the absence of exogenous zeitgebers in rats. PF-670462 (25, 50, and 100mg/kg, s.c.) induces dose-dependent phase shift. PF-670462 (50mg/kg; s.c.) significantly phase delays the rhythmic transcription of Bmal1, Per1, Per2 and Nr1d1 in both liver and pancreas by 4.5 ± 1.3 h and 4.5 ± 1.2 h, respectively, 1 day after administration. In the suprachiasmatic nucleus(SCN), the rhythm of Nr1d1 and Dbp mRNA expression is also delayed by 4.2 and 4 h, respectively.

 

推荐实验方法(仅供参考)

激酶实验:

Kinase Assay

The CKIε kinase assay is performed in a 40-μL final volume in buffer containing 50mM Tris, pH 7.5, 10mM MgCl2, 5mM dithiothreitol with 5μM ATP, 3nM CKIεΔ319, and 15μM peptide substrate PLSRTLpSVASLPGL in the presence of 5μL of CKIε inhibitor (PF-670462) or 5% dimethyl sulfoxide. The reaction is incubated for 3 h at 27°C; detection is carried out as described for the Kinase-Glo Assay. Luminescent output is measured.

 

动物实验:

 

Animal Administration

Adult male CD rats (initial weight 175-225 g) are released into constant darkness (DD) for 2 weeks, and their individual freerunning periods and times of activity onset are determined from the 7 to 10 days at the end of the 2-week period. Dosing of 50 mg/kg PF-670462 or vehicle (40% β-cyclodextrin) takes place at circadian time (CT)9 or 3 h before the predicted onset of activity; night vision goggles facilitated the subcutaneous administration. CT9 is chosen based on preliminary data demonstrating robust responses to CKIε inhibition at this circadian time. Animals are maintained under DD for an additional 4 to 5 days postdose, and the data from that time period are used in the estimation of the magnitude and direction of the putative phase shifts.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

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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

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):