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PF-431396 Sale

(Synonyms: N-甲基-N-[2-[[[2-[(2-氧代-2,3-二氢-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]苯基]甲磺酰胺) 目录号 : GC14407

A FAK/PYK2 dual inhibitor

PF-431396 Chemical Structure

Cas No.:717906-29-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥431.00
现货
10mg
¥609.00
现货
50mg
¥2,090.00
现货
200mg
¥4,935.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.IC50 value: 2 nM (FAK); 11 nM (PYK2); 445 nM (KD for BRD4) [1] [2]Target: FAK; PYK2; BRD4in vitro: PF-431396 is a potent and highly selective pyrimidine-based inhibitor of both Pyk2 and FAK, Consistent with the idea that the tyrosine phosphorylation of Pyk2 and FAK involves an initial autophosphorylation or transphosphorylation step, treating A20 cells with PF-431396 blocked anti-Ig-induced tyrosine phosphorylation of Pyk2 and FAK when the cells were stimulated in suspension when they were stimulated on ECM [3]. Nanomolar affinities were also determined for PF-431396 (Kd = 445 ± 42 nM) and for the PIM inhibitor (Kd = 565 ± 63 nM) [2].

References:
[1]. Buckbinder L, 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.
[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.

Chemical Properties

Cas No. 717906-29-1 SDF
别名 N-甲基-N-[2-[[[2-[(2-氧代-2,3-二氢-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]苯基]甲磺酰胺
化学名 N-methyl-N-[2-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide
Canonical SMILES CN(C1=CC=CC=C1CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C
分子式 C22H21F3N6O3S 分子量 506.5
溶解度 ≥ 18.1mg/mL in DMSO 储存条件 Store at -20°C
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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
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