化合物 PF-562271|T2465|TargetMol

PF-562271
717907-75-0

￥432 1mg 起订

￥977 5mg 起订

￥1530 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 PF-562271

英文名称：: PF-562271

CAS号：: 717907-75-0

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 97.65%

产品类别：: 抑制剂

货号：: T2465

Product Introduction

Bioactivity

名称	PF-562271
描述	PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
细胞实验	PF-562271 (Haoyuan Chemexpress Co., Ltd.) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or Dasatinib. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×103 Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC50 values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×103 cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction[2].
激酶实验	The purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer (50 mM HEPES pH 7.5, 125 mM NaCl, and 48 mM MgCl2) for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 M H2SO4). IC50 values are determined using the Hill-Slope Model[1].
体外活性	在胫骨植入MDA-MB-231细胞的大鼠中,口服 PF-562271（5 mg/kg）,引起骨钙素和松质骨增加,从而使肿瘤细胞生长减缓.在携带H125肺部异种移植肿瘤、异种移植PC3M-luc-C6的小鼠模型中,口服 PF-562271 （25 mg/kg）抑制肿瘤细胞生长,引起细胞凋亡.在U87 mg的小鼠中,PF-562271（口服< 33 mg/kg）能够以时间和剂量依赖的方式抑制肿瘤中FAK磷酸化.在BxPc3异种移植小鼠、PC3-M异种移植小鼠中口服 PF-562271（50 mg/kg）,能够抑制肿瘤生长.
体内活性	PF-562271能够结合在ATP与FAK结合的部位,并在激酶铰链区形成抑制剂与主链原子之间的氢键。在鸡胚绒毛尿囊膜中,PF-562271（1 nM ）阻断bFGF刺激的血管生成。在PC3-M细胞中,PF-562271（3.3 μM）能够使细胞停止在G1期。对于A431 细胞,PF-562271（250 nM ）能够抑制细胞侵入胶原蛋白。
存储条件	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 93 mg/mL (183.3 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	Cancer \| PTK2 \| Ewing \| Antitumor \| Pyk2 \| PTK2 protein tyrosine kinase 2 \| Sarcoma \| inhibit \| PF-562271 \| Breast \| FAK \| Focal adhesion kinase \| VS 6062 \| VS6062 \| Inhibitor \| Proline-rich tyrosine kinase 2 \| VS-6062
相关产品	Sodium Oxamate \| Ribociclib \| Palbociclib monohydrochloride \| Abemaciclib methanesulfonate \| CASIN \| Olomoucine \| Palbociclib \| GW 441756 \| Dinaciclib \| Defactinib \| Ro-3306 \| Abemaciclib
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

PF562271|||PF 562271|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子