貨號	規格	價格	上海	北京	武漢	南京
S81137-5mg	99.0%	￥560.00 S81137-5mg ￥560.00 現貨	6 6	-	-	-
S81137-10mg	99.0%	￥904.00 S81137-10mg ￥904.00 現貨	7 7	-	-	-
S81137-25mg	99.0%	￥1700.00 S81137-25mg ￥1700.00 現貨	6 6	-	-	-
S81137-100mg	≥98%	￥3700.00 S81137-100mg ￥3700.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively

產品描述：

PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively

靶點：

IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3);FAK;?PYK2;?CDK

體外研究：

PF-562271 (VS-6062) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength

體內研究：

PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo

參考文獻：

1. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944. 2. Lim ST, et al. FERM control of FAK function: implications for cancer therapy. Cell Cycle, 2008, 7(15), 2306-2314. 3. Canel M, et al. Quantitative in vivo imaging of the effects of inhibiting integrin signaling via Src and FAK on cancer cell movement: effects on E-cadherin dynamics. Cancer Res, 2010, 70(22), 9413-9422.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.502 ml	7.511 ml	15.023 ml
5 mM	0.3 ml	1.502 ml	3.005 ml
10 mM	0.15 ml	0.751 ml	1.502 ml
50 mM	0.03 ml	0.15 ml	0.3 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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PF-00562271 besylate