化合物 PF-04217903|T2676|TargetMol

PF-04217903
956905-27-4

￥233 1mg 起订

￥329 2mg 起订

￥538 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 PF-04217903

英文名称：: PF-04217903

CAS号：: 956905-27-4

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 98.55%

产品类别：: 抑制剂

货号：: T2676

Product Introduction

Bioactivity

Name	PF-04217903
Description	MET Tyrosine Kinase Inhibitor PF-04217903 is an orally bioavailabe, small-molecule tyrosine kinase inhibitor with potential antineoplastic activity.
Cell Research	Cells are treated with different concentrations PF-04217903 for 4 days. Cell proliferation is assessed by counting content of each well using a Coulter counter machine.(Only for Reference)
Kinase Assay	Cellular c-Met phosphorylation ELISA: A549 cells with endogenous human WT c-Met are seeded in 96-well plates in growth medium and cultured overnight. On the second day of the assay, the growth medium is replaced with serum-free medium (with 0.04% BSA). Serial dilutions of PF-04217903 are added to each well, and cells are incubated at 37 °C for 1 hour. Then 40 ng/mL HGF is added to the cells for 20 minutes. The cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells using lysis buffer. Phosphorylation of c-Met is assessed by an ELISA method utilizing capture antibodies specific for c-Met and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are incubated in the presence of protein lysates at 4 °C overnight and washed with 1% Tween 20 in PBS seven times. HRP-PY20 (horseradish peroxidase-conjugated anti-phosphotyrosine) is diluted 1:500 in blocking buffer and added to each plate for 30 minutes. Plates are then washed again, and TMB peroxidase substrate is added to initiate the HRP-dependent colorimetric reaction and the reaction stopped by addition of 0.09 N H2SO4. ELISA end points are the absorbance measured at 450 nm using a spectrophotometer. IC50 value is calculated by concentration-response curve fitting utilizing a Microsoft Excel-based four-parameter analytical met
In vitro	尽管在舒尼替尼敏感的B16F1和Tib6肿瘤模型中不能抑制肿瘤生长,但与单独使用舒尼替尼或PF-04217903相比,PF-04217903和舒尼替尼联用显著抑制舒尼替尼耐受性EL4和LLC肿瘤模型的肿瘤生长,血管扩张,表明舒尼替尼耐药肿瘤中HGF/c-Met轴的功能作用.
In vivo	PF-04217903明显抑制 LXFA 526L和LXFA 1647L克隆生长,IC50分别为16 nM和13 nM,与西妥昔单抗联用效果增强。PF-04217903有效抑制c-Met驱动的生物过程,如多种肿瘤细胞的生长,运动,侵袭和形态学变化。2 μM PF-04217903促进GTL-16 细胞死亡,其涉及磷酸化的4E-BP1,ERK/MAPK相关蛋白和 PI3K/AKT通路的下调。PF-04217903选择性比十字孢碱或PF-02341066高,PF-04217903作用于c-Met选择性比作用于其他一组208种激酶选择性高1000多倍,对c-Met致癌突变更敏感。除WT c-Met之外,PF-04217903显示出类似的抑制c-Met-H1094R,c-Met-R988C和c-Met-T1010I活性的效力,IC50为3.1 nM,6.4 nM和6.7 nM,但对c-Met-Y1230C没有抑制活性,IC50>10 μM。PF-04217903和舒尼替尼联用明显抑制内皮细胞增殖,但是不抑制肿瘤细胞B16F1,Tib6,EL4和LLC。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 20 mg/mL (53.71 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble)
Keywords	lung \| migration \| gastric \| GTL-16 \| PF-04217903 \| c-Met/HGFR \| inhibit \| phosphorylation \| colon \| PF 04217903 \| phospho-PDGFRβ \| PF04217903 \| carcinoma \| Inhibitor
Inhibitors Related	Capmatinib 2HCl \| Cabozantinib S-malate \| Crizotinib \| Amuvatinib \| (±)-Norcantharidin \| Capmatinib xHCl \| Capmatinib \| L-Ascorbic acid 2-phosphate trisodium \| SGI-7079 \| Norcantharidin \| Bacitracin Zinc \| AMG-458
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Highly Selective Inhibitor Library \| Tyrosine Kinase Inhibitor Library \| Drug Repurposing Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

PF-04217903|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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