| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D407963-1ml |
1ml |
现货  |
|
| 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 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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 |
| 产品介绍 |
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 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 lines：MCF-7 cells Concentrations：0-20 nM Incubation Time：72 hours Powder Purity:≥98% |
| IC50 | EGFR, IC50: 6.0 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=C(NC(=O)/C=C/CN2CCCCC2)C=C3C(=NC=NC3=C1)NC4=CC(=C(F)C=C4)Cl |
| 分子量 | 469.94 |
| 溶解性 | Solubility (25°C) In vitro Water: 51 mg/mL (199.93 mM); DMSO: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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