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PF-562271 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-562271 hydrochloride图片
CAS NO:939791-41-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
VS-6062(hydrochloride)
产品介绍
PF-562271 (VS-6062) hydrochloride 是一种有效,可逆,ATP 竞争性的FAKPyk2激酶抑制剂,IC50分别为 1.5 nM 和 13 nM。
生物活性

PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversibleFAKandPyk2kinase inhibitor withIC50s of 1.5 nM and 13 nM, respectively[1].

IC50& Target

IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)[1]

体外研究
(In Vitro)

PF-562271 (VS-6062) hydrochloride is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC50of 5 nM[1].
PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC50of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC50concentrations of 2.1 and 1.7 μM, respectively[2].

体内研究
(In Vivo)

PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC50of 93 ng/mL, total) after p.o. administration to tumor-bearing mice[1]. Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor[3].

分子量

543.95

Formula

C21H21ClF3N7O3S

CAS 号

939791-41-0

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.