1. Protein Tyrosine Kinase/RTK
  2. Pyk2
    FAK
  3. PF-431396

PF-431396 

目录号: HY-10460 纯度: 98.86%
产品使用指南

PF-431396 是具有口服活性的 FAKPyk2 的抑制剂,其 IC50 值分别为 2 nM 和 11 nM。

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PF-431396 Chemical Structure

PF-431396 Chemical Structure

CAS No. : 717906-29-1

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥990
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10 mg ¥900
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50 mg ¥2900
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100 mg ¥4800
In-stock
200 mg ¥8000
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500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products

    PF-431396 purchased from MCE. Usage Cited in: J Periodontal Res. 2015 Dec;50(6):855-863.

    PF431396 inhibits the phosphorylation of FAK and Akt.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively[1][2][3][4].

    IC50 & Target

    IC50: 2 nM (FAK); 11 nM (PYK2)[1].
    Kd: 445 nM (BRD4)[1].

    体外研究
    (In Vitro)

    PF-431396 has a Kd value of 445 nM for BRD4[2].
    PF-431396 appeares to selectively inhibit BCR-induced tyrosine phosphorylation of Pyk2 and FAK[3].
    PF-431396 (2.5, 5 μM, 45 min) inhibits the phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs[3].

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

    Western Blot Analysis[3]

    Cell Line: A20 cells ((105 cells in 0.5 ml of RPMI 1640 medium with 2% fetal calf serum and 50 μM 2-mercaptoethanol)).
    Concentration: 0.15, 1, 2.5, 5 μM.
    Incubation Time: 45 min.
    Result: The phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs was also inhibited.
    体内研究
    (In Vivo)

    PF-431396 (10 or 30 mg/kg, orally) prevents bone loss induced by estrogen deficiency in rats primarily by stimulating bone formation, providing independent pharmacological confirmation for the function of PYK2 in regulating bone formation[4].

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

    Animal Model: Sprague–Dawley female rats (ovariectomized (OVX) Rats)[4].
    Dosage: 10 or 30 mg/kg.
    Administration: Oral gavage, for 28 consecutive days.
    Result: Counteracted OVX-induced bone loss, completely preserving total bone content and total bone density.
    Promoted osteoblast recruitment and activity.
    分子量

    506.50

    Formula

    C22H21F3N6O3S

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    溶解性数据
    In Vitro: 

    DMSO : ≥ 100 mg/mL (197.43 mM)

    * "≥" 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 1.9743 mL 9.8717 mL 19.7433 mL
    5 mM 0.3949 mL 1.9743 mL 3.9487 mL
    10 mM 0.1974 mL 0.9872 mL 1.9743 mL
    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

    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.94 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.94 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    Inquiry Information

    产品名称:
    PF-431396
    目录号:
    HY-10460
    需求量: