Poziotinib
(Synonyms: 波齐替尼) 目录号 : GC17916
An inhibitor of EGFRs
Cas No.:1092364-38-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 values of 3.2, 5.3 and 23.5 nM for HER1, HER2 and HER4, respectively [1].
Epidermal growth factor receptors (EGFR/HER1, HER2/ErbB2, HER3/ErbB3, HER4/ErbB4) are receptor tyrosine kinases and play important roles in cell proliferation and differentiation. The EGFR family is a major target of anticancer drugs [1].
Poziotinib is an irreversible pan-HER inhibitor. In HER2 amplified SNU216 and N87 gastric cancer cells, HM781-36B inhibited cell growth with IC50 values of 4 and 1 nM, respectively. Also, HM781-36B potently inhibited the phosphorylation of HER family and downstream proteins such as STAT3, AKT and ERK, and induced G1 arrest and apoptosis. HM781-36B dose-dependently increased the amount of cleaved form of effector caspases (caspase-3 and caspase-7) and PARP, reduced antiapoptotic proteins BCL-2 and MCL-1, and induced proapoptotic protein BIM [1]. In HER2-amplified breast cancer cells, HM781-36B inhibited cell growth with IC50 values of 1, 1.2 and 9.5 nM for SK-BR-3, BT474, and MDA-MB-453 cells, respectively [2].
In nude mouse bearing N87 human gastric cancer xenograft model, HM781-36B significantly inhibited tumor growth and exhibited a synergistic effect when administered with chemotherapeutic agents [1].
References:
[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.
| Cas No. | 1092364-38-9 | SDF | |
| 别名 | 波齐替尼 | ||
| 化学名 | 1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one | ||
| 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 | ||
| 分子式 | C23H21Cl2FN4O3 | 分子量 | 491.34 |
| 溶解度 | ≥ 94.2mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0353 mL | 10.1763 mL | 20.3525 mL |
| 5 mM | 0.4071 mL | 2.0353 mL | 4.0705 mL |
| 10 mM | 0.2035 mL | 1.0176 mL | 2.0353 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。