计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Dacomitinib (PF299804, PF299)是一种有效的，不可逆的pan-ErbB抑制剂，最有效作用于EGFR，IC50为6 nM，高效作用于携带EGFR或ERBB2突变型(抗Gefitinib)和携带EGFR T790M突变型的NSCLCs。A potent and selective inhibitor of EGFR and ERBB phosphorylation.
Information
Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly toEGFRwithIC50of 6 nM in a cell-free assay. Dacomitinib inhibitsERBB2andERBB4with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EG
In vitro
PF299804 is a specific inhibitor of the ERBB family of kinases. PF299804 inhibits EGFR signaling and induces apoptosis in the EGFR T790M-containing H3255 GR cell line. PF299804 is effective in gefitinib-sensitive and gefitinibresistant NSCLC cell lines. PF299804 inhibits the growth of H3255 and HCC827 cells engineered to express EGFR T790M. PF299804 inhibits EGFR phosphorylation in the presence of the T790M mutation. PF-299804 is believed to irreversibly inhibit ERBB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of ERBB family members. PF299804 shows significant growth-inhibitory effects in HER2-amplified gastric cancer cells (SNU216, N87), and it has lower 50% inhibitory concentration values compared with other EGFR tyrosine kinase inhibitors, including gefitinib, lapatinib, BIBW-2992, and CI-1033. PF299804 induces apoptosis and G1 arrest and inhibits phosphorylation of receptors in the HER family and downstream signaling pathways including STAT3, AKT, and extracellular signal-regulated kinases (ERK) in HER2-amplified gastric cancer cells. PF299804 also blocks EGFR/HER2, HER2/HER3, and HER3/HER4 heterodimer formation as well as the association of HER3 with p85α in SNU216 cells. A recent research uses forty-seven human breast cancer and immortalized breast epithelial lines to evaluate the inhibition effects of PF299804, the results indicate PF299804 preferentially inhibits growth of HER-2-amplified breast cancer cell lines than nonamplified lines (RR = 3.39, p < 0.0001). PF299804 reduces the phosphorylation of HER2, EGFR, HER4, AKT, and ERK in the majority of sensitive lines. PF299804 exerts its anti-proliferative effect through a combined G0/G1 arrest and an induction of apoptosis.
In vivo
Orally administered PF299804 effectively inhibits growth of HCC827 Del/T790M xenografts. Low oral administration of PF-299804 (15mg/kg) causes significant antitumor activity, including marked tumor regressions in a variety of human tumor xenograft models that express and/ or overexpress ERBB family members or contain the double mutation (L858R/T790M) in ERBB1 (EGFR) associated with resistance to gefitinib and erlotinib.
Cell Data
cell lines：MCF-7 cells
Concentrations：0-20 nM
Incubation Time：72 hours
Powder Purity:≥98%
规格
英文别名
PF299804,PF299 | (E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide
规格或纯度
10mM in DMSO
英文名称
Dacomitinib (PF-00299804)
生化机理
达科米替（PF299804，PF299）是一种强效、不可逆的泛 ErbB 抑制剂，主要针对表皮生长因子受体，在无细胞试验中的 IC50 为 6 nM。达科米替尼抑制 ERBB2 和 ERBB4 的 IC50 分别为 45.7 nM 和 73.7 nM。达科米替尼对表皮生长因子受体（EGFR）或ERBB2突变（对吉非替尼耐药）以及表皮生长因子受体（EGFR）T790M突变的NSCLC有效。达科米替尼能抑制细胞生长并诱导细胞凋亡。第二阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
受体蛋白-酪氨酸激酶 erbB-4 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
分子量
469.94
Reaxy-Rn
24030737
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24030737&ln=
技术文档
高级数据
产品属性
| ALogP | 4.4 |
|---|
关联靶点（人）
ERBB4
Tclin
受体酪氨酸蛋白激酶 erbB-4(Receptor tyrosine-protein kinase erbB-4)
(0 活性数据)
ERBB2
Tclin
受体酪氨酸蛋白激酶 erbB-2(Receptor tyrosine-protein kinase erbB-2)
(1 活性数据)
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(12 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 51 mg/mL (199.93 mM); DMSO: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214639 |
分析证书 | D407963 |
技术文档和文章
溶液计算器
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