Dacomitinib-d10
Dacomitinib-d10 (PF-00299804-d10; PF-299804-d10) is the deuterated-labeled Dacomitinib (HY-13272). Dacomitinib (PF-00299804; PF-299804) is an orally active irreversible pan-ERBB receptor tyrosine kinase inhibitor with inhibitory activity against HER1/EGFR, HER2, and HER4. Dacomitinib 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 inhibits key signaling pathways such as PI3K‑AKT‑mTOR and PLK1‑FOXM1. Dacomitinib ameliorates pathological changes associated with pulmonary arterial hypertension in rats. Dacomitinib can be used in research on breast cancer, bladder cancer, epithelial ovarian cancer, and pulmonary arterial hypertension.
For research use only. We do not sell to patients.
- Formula: C24H15D10ClFN5O2
- Molecular Weight:480.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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CDK1 |
CDK2 |
Caspase-3 |
Caspase-7 |
Akt |
ERK |
EGFR |
HER1 6 nM (IC50) |
HER2 45.7 nM (IC50) |
HER4 73.7 nM (IC50) |
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 1110813-31-4
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Molecular Weight 480.00
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Formula C24H15D10ClFN5O2
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SMILES
COC(C(NC(/C=C/CN1C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C1([2H])[2H])=O)=C2)=CC3=C2C(NC4=CC(Cl)=C(C=C4)F)=NC=N3
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Synonyms
PF-00299804-d10; PF-299804-d10
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dacomitinib-d10 Related Classifications
HY-13272S3 Related Classifications
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Keywords
- Dacomitinib-d10
- PF-00299804-d10
- PF-299804-d10
- Isotope-Labeled Compounds
- EGFR
- IAP
- Akt
- ERK
- PI3K
- Survivin
- Caspase
- CDK
- Apoptosis
- Epidermal growth factor receptor
- ErbB-1
- HER1
- PKB
- Protein kinase B
- Extracellular signal regulated kinases
- Phosphoinositide 3-kinase
- Cyclin dependent kinase
- HER2-amplified breast cancer
- pulmonary arterial hypertension
- AsPC-1
- pancreatic ductal adenocarcinoma
- epithelial ovarian cancer
- PaTu 8902
- pan-ERBB receptor tyrosine kinase inhibitor
- PANC-1
- non-small cell lung cancer
- bladder cancer
- Inhibitor
- inhibitor
- inhibit