达克替尼|T2483

Dacomitinib
1110813-31-4

￥798 5瓶起订

￥1980 25瓶起订

￥4530 100瓶起订

￥315 1瓶起订

￥6360 200瓶起订

￥3180 50瓶起订

￥448 2瓶起订

￥835 1瓶起订

￥1120 10瓶起订

￥9450 500瓶起订

上海更新日期：2024-09-15

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 达克替尼

英文名称：: Dacomitinib

CAS号：: 1110813-31-4

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：: 99.34%

产品类别：: 抑制剂

货号：: T2483

Product Introduction

Bioactivity

名称	Dacomitinib
描述	Dacomitinib (PF299)(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
细胞实验	Growth and inhibition of growth is assessed by 5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay. This assay, a colorimetric method fordetermining the number of viable cells, is based on the bioreduction of MTS by cells to a formazan product that is soluble in cell culture medium, can be detected spectrophotometrically. The cells are exposed totreatment for 72 hours, and the number of cells used per experiment is determined empirically. All experimental points are set up in 6 to 12 wells, and all experiments are repeated at least thrice. The data are graphically displayed using GraphPad Prism version 3.00 for Windows (GraphPad Software). The curves are fitted using a nonlinear regression model with a sigmoidal dose response.(Only for Reference)
激酶实验	ELISA-Based ERBB Kinase Assay: The ERBB1, ERBB 2, and ERBB4 cytoplasmic fusion proteins are made by cloning the ERBB1 sequence (Met-668 to Ala-1211), ERBB2 (Ile-675 to Val-1256), and ERBB4 sequence (Gly-259 to Gly-690) into the baculoviral vector pFastBac using PCR. Proteins are expressed in baculovirusinfected Sf9 insect cells as GST fusion proteins. The proteins are purified by affinity chromatography using glutathione sepharose beads. Inhibition of ERBB tyrosine kinase activity is assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, 125 mM NaCl, 10 mM MgCl2, 100 μM sodium orthovanadate, 2 mM dithiothreitol, 20 μM ATP, PF299804 or vehicle control, and 1-5 nM GST-erbB per 50 μL of reaction mixture) are run in 96-well plates coated with 0.25 mg/mL poly-Glu-Tyr. The reactions are incubated for 6 minutes at room temperature while being shaken. Kinase reactions are stopped by removal of the reaction mixture, and then the wells are washed with wash buffer (0.1% Tween 20 in PBS). Phosphorylated tyrosine residues are detected by adding 0.2 μg/mL antiphosphotyrosine antibody (Oncogene Ab-4; 50 μL/well) coupled to horseradish peroxidase (HRP) diluted in PBS containing 3% BSA and 0.05% Tween 20 for 25 minutes while being shaken at room temperature. The antibody is removed, and plates are washed in wash buffer. HRP substrate (SureBlue3,3?,5,5?-tetramethyl benzidine or TMB) is added (50 μL per well) and incubated for 10-20 minutes while it is shaken at room temperature. The TMB reaction is stopped with the addition of 50 μL of stop solution (0.09 N H2SO4). The signal is quantified by measuring absorbance at 450 nm. IC50 values are determined for PF299804 using the median effect method.
体外活性	PF-299804（15 mg/kg,p.o.）具有较强的抗肿瘤活性.其可引起各种人肿瘤异种移植模型中明显的肿瘤退化,如表达和/或过表达ERBB家族成员,或与耐埃罗替尼和吉非替尼相关的含有双重突变(L858R/T790M)的ERBB1 (EGFR)异种移植模型.
体内活性	PF299804对EGFR信号传导有抑制作用,并可促使含EGFR T790M的H3255 GR细胞系凋亡。PF299804对表达T790M 突变体的H3255和 HCC827细胞的生长具有抑制作用。在HER2-扩增的胃癌细胞中,PF299804诱导细胞凋亡和G1期阻滞,并抑制HER家族及其下游信号通路,包括STAT3,AKT和细胞外信号调节激酶(ERK)中受体的磷酸化。PF299804还可阻断SNU216细胞中EGFR/HER2,HER2/HER3和HER3/HER4异质二聚体形成,以及HER3与p85α的结合。在大多数敏感细胞系中,PF299804对HER2,EGFR,HER4,AKT和ERK的磷酸化水平具有降低作用。PF299804通过G0/G1期阻滞和对细胞凋亡的诱导发挥其抗增殖作用。在47种人乳腺癌和永生的乳腺上皮细胞系中,相对于非扩增细胞系(RR = 3.39, p < 0.0001),PF299804优先抑制HER-2-扩增的乳腺癌细胞系的生长。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	1eq. HCl : 47 mg/mL (100 mM) DMSO : 45 mg/mL (95.76 mM)
关键字	Apoptosis \| PF 299 \| HER1 \| EGFR \| PF 00299804 \| PF299804 \| Epidermal growth factor receptor \| inhibit \| Inhibitor \| Dacomitinib \| PF 299804 \| PF-299 \| PF00299804 \| ErbB-1
相关产品	Gefitinib \| Metronidazole \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗癌活性化合物库 \| 抗癌上市药物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| EMA 上市药物库 \| FDA 上市激酶抑制剂库 \| 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

达克替尼|||PF-299804|||PF-00299804|||PF299

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