| 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 | HER2, IC50: 5.3 nM |
|---|---|
| ALogP | 5.046 |
| HBD Count | 1 |
| Rotatable Bond | 6 |
| Isomeric SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=C(C(=C(C=C3)Cl)Cl)F)OC4CCN(CC4)C(=O)C=C |
|---|---|
| PubChem CID | 25127713 |
| 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 |
|---|---|
| DMSO(mg / mL) Max Solubility | 98 |
| DMSO(mM) Max Solubility | 199.4545529 |
| Water(mg / mL) Max Solubility | ＜1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 |
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