PF-431396

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

PF-431396  纯度: 98.86%

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。

PF-431396

PF-431396 Chemical Structure

CAS No. : 717906-29-1

规格 价格 是否有货 数量
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   询价  
1 g   询价  

* Please select Quantity before adding items.

PF-431396 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library

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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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

717906-29-1

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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Seungil Han, et al. Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design. J Biol Chem. 2009 May 8; 284(19): 13193–13201.

    [2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2.

    [3]. Tse KW, et al. B cell receptor-induced phosphorylation of Pyk2 and focal adhesion kinase involves integrins and the Rap GTPases and is required for B cell spreading. J Biol Chem. 2009 Aug 21;284(34):22865-77.

    [4]. Leonard Buckbinder, et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10619-24.

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