PF-562271 HCl

PF-562271 (VS-6062) hydrochloride 是一种有效的 ATP 竞争性和可逆的 FAK 和 Pyk2 激酶抑制剂，IC50 分别为 1.5 nM 和 13 nM。

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库存: 现货

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价格

促销价

数量
5mg

￥1037.00

830.00

- +
10mg

￥1575.00

1260.00

- +
50mg

￥4237.00

3390.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci5862
CAS: 939791-41-0
别名: PF562271 HCl;PF 562271 HCl
分子式: C21H21ClF3N7O3S
分子量: 543.95
纯度: >98%
溶解度: ≥ 26.35mg/mL in DMSO with gentle warming
储存: Store at -20°C
库存: 现货

Background

PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.

参考文献:
[1]Stokes JB, Adair SJ, Slack-Davis JK, Walters DM, Tilghman RW, Hershey ED, Lowrey B, Thomas KS, Bouton AH, Hwang RF, Stelow EB, Parsons JT, Bauer TW. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45. doi: 10.1158/1535-7163.MCT-11-0261. Epub 2011 Sep 8.
[2]Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.