1. Cell Cycle/DNA Damage Stem Cell/Wnt
  2. Casein Kinase
  3. PF-670462 dihydrochloride

PF-670462 dihydrochloride 

目录号: HY-15490 纯度: 99.96%
COA 产品使用指南

PF-670462 dihydrochloride 是一种有效的,选择性的 casein kinase (CKIε/CKIδ) 抑制剂,IC50 值分别为 7.7 nM 和 14 nM。

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PF-670462 dihydrochloride Chemical Structure

PF-670462 dihydrochloride Chemical Structure

CAS No. : 950912-80-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1351
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1 mg ¥319
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5 mg ¥767
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10 mg ¥1216
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25 mg ¥2346
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50 mg ¥3753
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100 mg ¥5254
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products

    PF-670462 dihydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Mar 12;523(3):809-815.  [Abstract]

    Immunoblot analysis of cells treated with IC261 or PF670462 for 48 h. GAPDH served as a loading control.

    PF-670462 dihydrochloride purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    CK1ε phosphorylates LRP6 at Thr1479 in vitro and TPA enhances the kinase activity of CK1ε. GST-LRP6 mini fragment fusion protein is incubated with recombinant CK1ε in the presence of 200 μM ATP with or without 160 μM TPA or 2 μM PF670462 as indicated.

    查看 Casein Kinase 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

    IC50 & Target[1]

    CKIδ

    14 nM (IC50)

    EGFR

    150 nM (IC50)

    SAPK2A/p38

    190 nM (IC50)

    体外研究
    (In Vitro)

    PF-670462 is a potent and selective inhibitor of CKIε and CKIδ, with IC50s of 7.7 nM and 14 nM, respectively. PF-670462 shows less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC50s of 150 nM and 190 nM, respectively. PF-670462 also causes a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC50 of 290 ± 39 nM in CKIε-transfected COS7 cells[1]. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC50 of ∼17 nM. PF-670462 (1 μM) is a weak inhibitor of proliferation, and only modestly suppresses the growth of HEK293 and HT1080 cells. PF-670462 (100 nM) strongly inhibits CK1ε and CK1δ, consistent with its effect on Wnt/β-catenin signaling[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    PF-670462 (50 mg/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 100 mg/kg, s.c.) induces dose-dependent phase shift[1]. PF-670462 (50 mg/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[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    410.32

    Formula

    C19H22Cl2FN5

    CAS 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 100 mg/mL (243.71 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 32 mg/mL (77.99 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4371 mL 12.1856 mL 24.3712 mL
    5 mM 0.4874 mL 2.4371 mL 4.8742 mL
    查看完整储备液配制表

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.07 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.07 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 25 mg/mL (60.93 mM); 澄清溶液; 超声助溶 (<60°C)

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.96%

    参考文献
    Kinase Assay
    [1]

    The CKIε kinase assay is performed in a 40-μL final volume in buffer containing 50 mM Tris, pH 7.5, 10 mM MgCl2, 5 mM dithiothreitol with 5 μM ATP, 3 nM CKIεΔ319, and 15 μM peptide substrate PLSRTLpSVASLPGL in the presence of 5 μL 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Adult male CD rats (initial weight 175-225 g) are released into constant darkness (DD) for 2 weeks, and their individual free-running 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    PF-670462 dihydrochloride 相关分类

    完整储备液配制表

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.4371 mL 12.1856 mL 24.3712 mL 60.9281 mL
    5 mM 0.4874 mL 2.4371 mL 4.8742 mL 12.1856 mL
    10 mM 0.2437 mL 1.2186 mL 2.4371 mL 6.0928 mL
    15 mM 0.1625 mL 0.8124 mL 1.6247 mL 4.0619 mL
    20 mM 0.1219 mL 0.6093 mL 1.2186 mL 3.0464 mL
    25 mM 0.0975 mL 0.4874 mL 0.9748 mL 2.4371 mL
    30 mM 0.0812 mL 0.4062 mL 0.8124 mL 2.0309 mL
    40 mM 0.0609 mL 0.3046 mL 0.6093 mL 1.5232 mL
    50 mM 0.0487 mL 0.2437 mL 0.4874 mL 1.2186 mL
    60 mM 0.0406 mL 0.2031 mL 0.4062 mL 1.0155 mL
    H2O 80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7616 mL
    100 mM 0.0244 mL 0.1219 mL 0.2437 mL 0.6093 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
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