Dacomitinib-d10 dihydrochloride
Dacomitinib-d10 dihydrochloride (PF-00299804-d10 dihydrochloride; PF-299804-d10 dihydrochloride) 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: C24H17D10Cl3FN5O2
- Molecular Weight:552.92
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Appearance Solid
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Molecular Weight 552.92
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Formula C24H17D10Cl3FN5O2
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Color White to off-white
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SMILES
O=C(/C=C/CN1C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C1([2H])[2H])NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F.[H]Cl.[H]Cl
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Synonyms
PF-00299804-d10 dihydrochloride; PF-299804-d10 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 dihydrochloride Related Classifications
HY-13272S2 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
- 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