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

PF-431396 

目录号: HY-10460 纯度: 99.15%
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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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥990 In-stock
10 mg ¥900 In-stock
50 mg ¥2900 In-stock
100 mg ¥4800 In-stock
200 mg ¥8000 In-stock
500 mg   Get quote  
1 g   Get quote  

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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

    Description

    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].

    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].

    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.
    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].

    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.
    Molecular Weight

    506.50

    Formula

    C₂₂H₂₁F₃N₆O₃S

    CAS No.

    717906-29-1

    SMILES

    CS(=O)(N(C)C1=CC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (197.43 mM)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *

    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。 -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。

    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。
    References
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    The molarity calculator equation

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    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    PF-431396PF431396PF 431396Pyk2FAKProline-rich tyrosine kinase 2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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