| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P407902-1ml |
1ml |
现货  |
|
| 英文别名 | NOV120101 | 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Poziotinib (HM781-36B) |
| 生化机理 | 波唑替尼（HM781-36B，NOV120101）是一种不可逆的泛 HER 抑制剂，对 HER1、HER2 和 HER4 的 IC50 分别为 3.2 nM、5.3 nM 和 23.5 nM。Poziotinib 还能诱导细胞凋亡和 G1 细胞周期停滞。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 | 表皮生长因子受体抑制剂 |
| 产品介绍 |
Information Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HERinhibitor withIC50of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also inducesapoptosisand G1 cell cycle arrest. Phase 2. Poziotinib specifically inhibits the cell growth in HER2 amplified gastric cancer cells, and inhibits the phosphorylation of EGFR and key components of downstream signaling cascades such as STAT3, AKT and ERK. Poziotinib also induces apoptosis and G1 cell cycle arrest by activating the mitochondrial pathway in HER2 amplified gastric cancer cells. Furthermore, Poziotinib also exerts synergistic effects with chemotherapeutic agents in both HER2 amplified and HER2 non-amplified gastric cancer cells. In vivo In nude mice bearing N87 human gastric cancer xenografts, Poziotinib (0.5 mg/kg p.o.) alone significantly inhibits the growth of tumors, and coadministraion of Poziotinib and 5-FU causes more effective tumor inhibition. In addition, HM781-36B shows excellent antitumor activity in a variety of EGFR- and HER-2-dependent tumor xenograft models, including erlotinib-sensitive HCC827 NSCLC cells, erlotinib-resistant NCI-H1975 NSCLC cells, HER-2 overexpressing Calu-3 NSCLC cells, NCI-N87 gastric cancer cells, SK-Ov3 ovarian cancer cells and EGFR-overexpressing A431 epidermoid carcinoma cancer cells. cell lines： Concentrations：~10 μM Incubation Time：72 hours Powder Purity:≥97% |
| IC50 | HER1, IC50: 3.2 nM |
|---|
| Canonical SMILES | COC1=CC2=C(C=C1OC3CCN(CC3)C(=O)C=C)C(=NC=N2)NC4=CC=C(Cl)C(=C4F)Cl |
|---|---|
| 分子量 | 491.34 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 51 mg/mL (200.56 mM); Water: Insoluble; Ethanol: 51 mg/mL |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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