1042385-75-0
Chemical Structure
Dacomitinib hydrate
Synonym(s): PF-00299804 hydrate; PF-299804 hydrate
- CAS No.: 1042385-75-0
- Formula:C24H27ClFN5O3
- Molecular Weight:487.95
IUPAC Name: (E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide hydrate
InChIKey: BSPLGGCPNTZPIH-IPZCTEOASA-N
SMILES: O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F.O
Biological Activity: Dacomitinib hydrate (PF-00299804 hydrate; PF-299804 hydrate) is an orally active irreversible pan-ERBB receptor tyrosine kinase inhibitor with inhibitory activity against HER1/EGFR, HER2, and HER4. Dacomitinib hydrate exerts antitumor effects in various tumor cells, inhibiting tumor cell proliferation, migration, and invasion, inducing cell cycle arrest and apoptosis, regulating the expression of molecules related to the cell cycle, apoptosis, and epithelial-mesenchymal transition, and it can also reverse partial drug resistance, producing synergistic effects when combined with chemotherapy. Dacomitinib hydrate inhibits key signaling pathways such as PI3K‑AKT‑mTOR and PLK1‑FOXM1. Dacomitinib hydrate ameliorates pathological changes associated with pulmonary arterial hypertension in rats. Dacomitinib hydrate can be used in research on breast cancer, bladder cancer, epithelial ovarian cancer, and pulmonary arterial hypertension[1][2][3][4][5][6][7][8].
| Cat. No. | Nom du produit | Pureté | Description | Pricing | |||||||||||||||||||
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Dacomitinib hydrate | 99.54% | Dacomitinib hydrate (PF-00299804 hydrate; PF-299804 hydrate) is an orally active irreversible pan-ERBB receptor tyrosine kinase inhibitor with inhibitory activity against HER1/EGFR, HER2, and HER4. Dacomitinib hydrate exerts antitumor effects in various tumor cells, inhibiting tumor cell proliferation, migration, and invasion, inducing cell cycle arrest and apoptosis, regulating the expression of molecules related to the cell cycle, apoptosis, and epithelial-mesenchymal transition, and it can also reverse partial drug resistance, producing synergistic effects when combined with chemotherapy. Dacomitinib hydrate inhibits key signaling pathways such as PI3K‑AKT‑mTOR and PLK1‑FOXM1. Dacomitinib hydrate ameliorates pathological changes associated with pulmonary arterial hypertension in rats. Dacomitinib hydrate can be used in research on breast cancer, bladder cancer, epithelial ovarian cancer, and pulmonary arterial hypertension. | ||||||||||||||||||||
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Similarity Score 0.99
HY-13272Dacomitinib -
Similarity Score 0.89
HY-Z4786Dacomitinib impurity 1 -
Similarity Score 0.88
HY-160828O-Desmethyl dacomitinib -
Similarity Score 0.79
HY-Z4779Dacomitinib impurity 4 -
Similarity Score 0.79
HY-153111EGFR/HER2-IN-9 -
Similarity Score 0.77
HY-101450PF-6274484 -
Similarity Score 0.76
HY-164503Neptinib -
Similarity Score 0.75
HY-Z2264Afatinib impurity 36 -
Similarity Score 0.75
HY-138916PF-06672131 -
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References
- [1]. Momeny M, et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells. Cellular oncology (Dordrecht, Netherlands). 2019 Aug;42(4):491-504.
- [2]. Grivas PD, et al. Evaluation of the antitumor activity of dacomitinib in models of human bladder cancer. Molecular medicine (Cambridge, Mass.). 2013 Nov 08;19(1):367-76.
- [3]. Reckamp KL, et al. A phase 2 trial of dacomitinib (PF-00299804), an oral, irreversible pan-HER (human epidermal growth factor receptor) inhibitor, in patients with advanced non-small cell lung cancer after failure of prior chemotherapy and erlotinib. Cancer. 2014 Apr 15;120(8):1145-54.
- [4]. Shirley M, et al. Dacomitinib: First Global Approval. Drugs. 2018 Dec;78(18):1947-1953.
- [5]. Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib. Molecular cancer therapeutics. 2012 Sep;11(9):1978-87. [Content Brief]
- [6]. Momeny M, et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells. Scientific reports. 2017 Jun 23;7(1):4204.
- [7]. Yu X, et al. Dacomitinib, a new pan-EGFR inhibitor, is effective in attenuating pulmonary vascular remodeling and pulmonary hypertension. European journal of pharmacology. 2019 May 05;850:97-108.
- [8]. Van Sebille YZA, et al. Dacomitinib-induced diarrhoea is associated with altered gastrointestinal permeability and disruption in ileal histology in rats. International journal of cancer. 2017 Jun 15;140(12):2820-2829.
