Poziotinib
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Poziotinib (HM781-36B)是一个不可逆的pan-HER抑制剂,对HER1\HER2和HER4的IC50值分别是3.2\5.3和23.5 nM[1].
表皮生长因子受体是受体酪氨酸激酶,包含EGFR/HER1\HER2/ErbB2\HER3/ErbB3和HER4/ErbB4,在细胞增殖和分化中发挥重要作用.EGFR家族是抗癌药物的主要靶点[1].
Poziotinib是一个不可逆的pan-HER抑制剂.在HER2扩增的SNU216和N87胃癌细胞中,HM781-36B抑制细胞生长,IC50值分别为4和1 nM.此外,HM781-36B有效抑制HER家族和下游蛋白的磷酸化,如STAT3\AKT和ERK,并诱导G1阻滞和细胞凋亡.HM781-36B以剂量依赖性方式增加效应caspases (caspase-3和caspase-7)以及PARP的切割形式的含量,降低抗凋亡蛋白BCL-2和MCL-1,并诱导促凋亡蛋白BIM[1].在HER2扩增的乳腺癌细胞中,HM781-36B抑制SK-BR-3\BT474和MDA-MB-453细胞的生长,IC50值分别为1\1.2和9.5 nM[2].
在N87人胃癌异种移植裸鼠模型中,HM781-36B显著抑制肿瘤生长,与化疗剂给药表现出协同效应[1].
参考文献：
[1]. Nam HJ, Kim HP, Yoon YK, et al. Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett, 2011, 302(2): 155-165.
[2]. Kim HJ, Kim HP, Yoon YK, et al. Antitumor activity of HM781-36B, a pan-HER tyrosine kinase inhibitor, in HER2-amplified breast cancer cells. Anticancer Drugs, 2012, 23(3): 288-297.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 491.34 |
| Cas No. | 1092364-38-9 |
| Formula | C23H21Cl2FN4O3 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥94.2 mg/mL in DMSO |
| Chemical Name | 1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one |
| SDF | Download SDF |
| Canonical SMILES | C=CC(N1CCC(OC2=C(OC)C=C3C(C(NC4=C(F)C(Cl)=C(Cl)C=C4)=NC=N3)=C2)CC1)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
