PF-431396
目录号 : KM2606 CAS No. : 717906-29-1 纯度 : 98%

PF-431396 是具有口服活性的 FAK 和Pyk2 的抑制剂,其 IC50 值分别为 2 nM 和 11 nM。

规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg
In-stock
500mg 询价 In-stock
1g 询价 In-stock

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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.

体外研究

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

Western Blot Analysis

Cell Line: A20 cells ((10 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

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.

Animal Model: Sprague–Dawley female rats (ovariectomized (OVX) Rats).
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.
分子式
C22H21F3N6O3S
分子量
506.50
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。

  • 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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