|N-甲基-N-(3-(2-((2-氧代吲哚-5-基)氨基)-5-(三氟甲基)嘧啶-4-基)氨基)甲基)吡啶-2-基)甲烷磺酰胺苯磺酸盐|CsnPharm

CAS No.: 939791-38-5

PF-562271 besylate/PF 562271 苯磺酸盐 Catalog No. CSN13737

Synonyms: VS-6062 besylate

PF-562271 besylate is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and > 100-fold selectivity against other protein kinases, except for some CDKs.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述FAK (Focal adhesion kinase), a non-receptor tyrosine kinase, can regulate the cytoskeleton and act as a scaffolding and signaling protein for other adhesion molecules. The expression of FAK and its phosphorylation status show a strong correlation with the invasive phenotype of aggressive human tumors. PF-562271 Besylate is the besylate form of PF-562271. PF-562271 is a potent and selective inhibitor for FAK and Pyk2 with IC50 values of 1.5nM and 14nM (measured by recombinant kinase assay), respectively, displaying over 100-fold selectivity against the other kinases tested^[1]. PF-562271 showed robust inhibition on p-FAK with IC50 of 5nM in an inducible cell-based assay. Oral administration of PF-562271 can inhibit p-FAK in a dose-dependent fashion with calculated EC50 of 93ng/ml in the tumor-bearing mice, which suggesting the pharmacodynamics of this compound. In vitro study showed that PF-562271 had antitumor efficacy or caused tumor regression in multiple human s.c. xenograft models, including BxPC3, LoVo, U87MG, H125, PC3M and BT474, with dose ranging in 25-100mg/kg according to different models^[1].
作用机制PF-562271 can bind in the ATP-binding cleft of FAK and form two of the three H-bonds between PF-562271 and main-chain atoms in the kinase hinge region.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
ALL-PO cell	-	Growth inhibition assay	-	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.01584 μM	SANGER
human 8305C cell	-	Growth inhibition assay	-	Inhibition of human 8305C cell growth in a cell viability assay, IC50=1.09904 μM	SANGER
human AGS cell	-	Growth inhibition assay	-	Inhibition of human AGS cell growth in a cell viability assay, IC50=1.52124 μM	SANGER

更多
动物研究
剂量
Mice: 12 mg/kg - 50 mg/kg^[1] (p.o.) Monkey: 20 mg/kg - 80 mg/kg^[2] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 12 mg/kg - 50 mg/kg^[1] (p.o.) Monkey: 20 mg/kg - 80 mg/kg^[2] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5023 mL
- 7.5113 mL
- 15.0226 mL
- 5 mM
- 0.3005 mL
- 1.5023 mL
- 3.0045 mL
- 10 mM
- 0.1502 mL
- 0.7511 mL
- 1.5023 mL

技术信息

CAS号

939791-38-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H26F3N7O6S2

运输

蓝冰

分子量

665.66

别名

VS-6062 besylate

溶解度

DMSO	150.0 mg/mL (225.3 mM)
Water	insoluble

动物实验配方

4% DMSO+30% PEG 300+water

3 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

ALL-PO cell	-	Growth inhibition assay	-	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.01584 μM	SANGER
human 8305C cell	-	Growth inhibition assay	-	Inhibition of human 8305C cell growth in a cell viability assay, IC50=1.09904 μM	SANGER
human AGS cell	-	Growth inhibition assay	-	Inhibition of human AGS cell growth in a cell viability assay, IC50=1.52124 μM	SANGER
human AN3-CA cell	-	Growth inhibition assay	-	Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=1.21867 μM	SANGER
human BC-1 cell	-	Growth inhibition assay	-	Inhibition of human BC-1 cell growth in a cell viability assay, IC50=1.61664 μM	SANGER
human BCPAP cell	-	Growth inhibition assay	-	Inhibition of human BCPAP cell growth in a cell viability assay, IC50=1.01288 μM	SANGER
human BPH-1 cell	-	Growth inhibition assay	-	Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=1.28766 μM	SANGER
human CAL-33 cell	-	Growth inhibition assay	-	Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=1.12938 μM	SANGER
human CAL-62 cell	-	Growth inhibition assay	-	Inhibition of human CAL-62 cell growth in a cell viability assay, IC50=1.31909 μM	SANGER
human CGTH-W-1 cell	-	Growth inhibition assay	-	Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=1.61679 μM	SANGER
human COLO-205 cell	-	Growth inhibition assay	-	Inhibition of human COLO-205 cell growth in a cell viability assay, IC50=0.48658 μM	SANGER
human COLO-829 cell	-	Growth inhibition assay	-	Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.76176 μM	SANGER
human DU-145 cell	-	Growth inhibition assay	-	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=2.49118 μM	SANGER
human DU-4475 cell	-	Growth inhibition assay	-	Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=2.14759 μM	SANGER
human EW-13 cell	-	Growth inhibition assay	-	Inhibition of human EW-13 cell growth in a cell viability assay, IC50=1.63466 μM	SANGER
human HSC-2 cell	-	Growth inhibition assay	-	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.5395 μM	SANGER
human HUTU-80 cell	-	Growth inhibition assay	-	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.44886 μM	SANGER
human IGROV-1 cell	-	Growth inhibition assay	-	Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.81038 μM	SANGER
human KM12 cell	-	Growth inhibition assay	-	Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.38557 μM	SANGER
human KYSE-150 cell	-	Growth inhibition assay	-	Inhibition of human KYSE-150 cell growth in a cell viability assay, IC50=1.35236 μM	SANGER
human KYSE-270 cell	-	Growth inhibition assay	-	Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=1.04714 μM	SANGER
human MDA-MB-231 cell	-	Growth inhibition assay	-	Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=2.49572 μM	SANGER
human MES-SA cell	-	Growth inhibition assay	-	Inhibition of human MES-SA cell growth in a cell viability assay, IC50=1.30682 μM	SANGER
human MFE-296 cell	-	Growth inhibition assay	-	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=2.47792 μM	SANGER
human MG-63 cell	-	Growth inhibition assay	-	Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.80637 μM	SANGER
human MZ1-PC cell	-	Growth inhibition assay	-	Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=1.62312 μM	SANGER
human NCI-H460 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=2.04839 μM	SANGER
human NCI-H650 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=0.83154 μM	SANGER
human NKM-1 cell	-	Growth inhibition assay	-	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.27506 μM	SANGER
human RT-112 cell	-	Growth inhibition assay	-	Inhibition of human RT-112 cell growth in a cell viability assay, IC50=0.9846 μM	SANGER
human SIG-M5 cell	-	Growth inhibition assay	-	Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=1.48487 μM	SANGER
human SK-UT-1 cell	-	Growth inhibition assay	-	Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=1.44647 μM	SANGER
human SNU-387 cell	-	Growth inhibition assay	-	Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=2.5282 μM	SANGER
human ST486 cell	-	Growth inhibition assay	-	Inhibition of human ST486 cell growth in a cell viability assay, IC50=1.53278 μM	SANGER
human SW1710 cell	-	Growth inhibition assay	-	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.62628 μM	SANGER
human SW982 cell	-	Growth inhibition assay	-	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.3282 μM	SANGER
human U251 cell	-	Growth inhibition assay	-	Inhibition of human U251 cell growth in a cell viability assay, IC50=1.74031 μM	SANGER
MV-4-11 cell	-	Growth inhibition assay	-	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.2766 μM	SANGER
NCI-H810 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=1.10776 μM	SANGER

PF-562271 besylate/PF 562271 苯磺酸盐 Catalog No. CSN13737

靶点选择性

请登录您的专属账户

确认信息