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Poziotinib
- HM781-36B
- Soluble in DMSO
- MF: C23H21Cl2FN4O3
- MW: 491.34
Description
Poziotinib is an irreversible pan-HER inhibitor with IC50 values of 0.0032 µM, 0.0053 µM and 0.0235 µM for HER1, HER2 and HER4, respectively. Poziotinib inhibited phosphorylation of HER family and downstream signaling molecules, and induced apoptosis and G1 arrest. Moreover, poziotinib demonstrated potent antitumor activity in HER2 amplified gastric cancer cells, HER2-amplified breast cancer cells, and erlotinib-resistant NSCLC.
More Information
| Parent CAS No. | 1092364-38-9 |
|---|---|
| Chemical Name | 1-(4-(4-(3,4-Dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one |
| SMILES | C1CC(OC2C=C3C(NC4C=CC(Cl)=C(Cl)C=4F)=NC=NC3=CC=2OC)CCN1C(C=C)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29) |
| InChiKey | LPFWVDIFUFFKJU-UHFFFAOYSA-N |
| CID | 25127713 |
| Short Description | HER inhibitor |
References
- HJ Nam 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 Mar 28;302(2):155-65.
- MY Cha et al. Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54.
- HJ Kim et al. Antitumor activity of HM781-36B, a pan-HER tyrosine kinase inhibitor, in HER2-amplified breast cancer cells. Anticancer Drugs. 2012 Mar;23(3):288-97.
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