Dacomitinib hydrate
Based on 29 publication(s) in Google Scholar
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.54%
- CAS No.: 1042385-75-0
- Formule: C24H27ClFN5O3
- Masse moléculaire:487.95
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Dacomitinib hydrate
More- Cancer Res. 2025 Dec 29. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
- Adv Sci (Weinh). 2025 Nov 9:e07524. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Pharmacol Res. 2025 Nov:221:107993. [Abstract]
- EMBO J. 2024 Apr;43(8):1388-1419. [Abstract]
- Stem Cell Res Ther. 2024 Jul 18;15(1):217. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]
- RSC Adv. 2025 Dec 18;15(59):50944-50962. [Abstract]
- RSC Adv. 2018 Nov 19;8(68):38733-38744. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Front Chem. 2020 Jul 28;8:596. [Abstract]
- ACS Omega. 2023 Jun 14;8(25):22603-22612. [Abstract]
- Molecules. 2024 Jan 4;29(1):274. [Abstract]
- Sci Rep. 2024 May 9;14(1):10662. [Abstract]
- Oncol Rep. 2026 Feb;55(2):30. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- BMC Bioinformatics. 2023 May 24;24(1):215. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- PLoS One. 2019 Apr 4;14(4):e0214598. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Biochem Biophys Res Commun. 2026 Feb 12:800:153165.
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- bioRxiv. 2025 May 10.
- bioRxiv. 2023 Dec 12.
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- bioRxiv. 2020 Jun.
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
46 nM
Compound: 25, PF-00299804
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Inhibition of GST-tagged ErbB2 expressed in sf9 cells by ELISA
Inhibition of GST-tagged ErbB2 expressed in sf9 cells by ELISA
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[PMID: 22621397] |
| Sf9 | IC50 |
6 nM
Compound: 25, PF-00299804
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Inhibition of GST-tagged EGFR expressed in sf9 cells by ELISA
Inhibition of GST-tagged EGFR expressed in sf9 cells by ELISA
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[PMID: 22621397] |
| Sf9 | IC50 |
74 nM
Compound: 25, PF-00299804
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Inhibition of GST-tagged ErbB4 expressed in sf9 cells by ELISA
Inhibition of GST-tagged ErbB4 expressed in sf9 cells by ELISA
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[PMID: 22621397] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1042385-75-0
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Appearance Solid
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Masse moléculaire 487.95
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Formule C24H27ClFN5O3
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Color White to light yellow
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SMILES
O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F.O
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Synonyms
PF-00299804 hydrate; PF-299804 hydrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (29)
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Journal Impact Factor
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Most Recent
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Cancer Res
2025 Dec 29. PMID: 41460723 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Exp Clin Cancer Res
Pyrotinib targeted EGFR/GRP78 mediated cell apoptosis in high EGFR gene copy number gastric cancer. [Abstract]2025 Aug 19;44(1):245. PMID: 40830980
Dacomitinib hydrate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Aug 19;44(1):245. [Abstract]
Primary gastric cancer (GC-1 and GC-2) cells treated with Pyrotinib, Dacomitinib, Afatinib, or DMSO (control) at 1 µM concentration over 3 days, growth curves represent three independent experiments.
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Adv Sci (Weinh)
Amphiregulin and Epiregulin Confer Radioresistance in Esophageal Squamous Cell Carcinoma Through Oxidative Phosphorylation. [Abstract]2025 Nov 9:e07524. PMID: 41208199
Dacomitinib hydrate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 9:e07524. [Abstract]
Dacomitinib (7 mg/kg, i.g.) largely improved the radiosensitivity of subcutaneous xenograft tumors.
Dacomitinib hydrate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 9:e07524. [Abstract]
The combination of Dacomitinib (7 mg/kg, i.g.) and IR induced much more cell death than either IR or dacomitinib alone.
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Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Pharmacol Res
Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]2025 Nov:221:107993. PMID: 41083089 -
EMBO J
The growth factor EPIREGULIN promotes basal progenitor cell proliferation in the developing neocortex. [Abstract]2024 Apr;43(8):1388-1419. PMID: 38514807 -
Stem Cell Res Ther
Transplantation of human endometrial perivascular stem cells with hydroxy saffron yellow A promotes uterine repair in rats. [Abstract]2024 Jul 18;15(1):217. PMID: 39020406 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Mol Cancer Ther
Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]2018 Mar;17(3):603-613. PMID: 29237806 -
RSC Adv
Integrative machine learning-guided in silico and in vitro approach reveals selective small molecule inhibitors targeting mutant IDH1. [Abstract]2025 Dec 18;15(59):50944-50962. PMID: 41426059 -
RSC Adv
Characterization of reactive intermediates formation in dacomitinib metabolism and bioactivation pathways elucidation by LC-MS/MS: in vitro phase I metabolic investigation. [Abstract]2018 Nov 19;8(68):38733-38744. PMID: 35558335 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Front Chem
Deducing the Conformational Properties of a Tyrosine Kinase Inhibitor in Solution by Optical Spectroscopy and Computational Chemistry. [Abstract]2020 Jul 28;8:596. PMID: 32850633 -
ACS Omega
2023 Jun 14;8(25):22603-22612. PMID: 37387790 -
Molecules
Pan-EGFR Inhibitor Dacomitinib Resensitizes Paclitaxel and Induces Apoptosis via Elevating Intracellular ROS Levels in Ovarian Cancer SKOV3-TR Cells. [Abstract]2024 Jan 4;29(1):274. PMID: 38202856
Dacomitinib hydrate purchased from MedChemExpress. Usage Cited in: Molecules. 2024 Jan 4;29(1):274. [Abstract]
SKOV3-TR cells were treated with combination of Dacomitinib (0, 0.1, 0.5, and 1 µM) and Paclitaxel (0, 10, 100, and 200 nM) as indicated for 48 h, and then cleaved PARP was analyzed by immunoblotting.
Dacomitinib hydrate purchased from MedChemExpress. Usage Cited in: Molecules. 2024 Jan 4;29(1):274. [Abstract]
SKOV3-TR cells were subjected to treatments with DMSO (Mock), 200 nM paclitaxel, 1 µM Dacomitinib, and combination of 200 nM Paclitaxel and 1 µM Dacomitinib each for 48 h. Apoptotic cell death was analyzed by FACS analysis.
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Sci Rep
The prognostic significance and potential mechanism of DBF4 zinc finger in hepatocellular carcinoma. [Abstract]2024 May 9;14(1):10662. PMID: 38724606 -
Oncol Rep
Inhibition of primary ciliogenesis enhances efficacy of EGFR‑TKIs against non‑small cell lung cancer cells. [Abstract]2026 Feb;55(2):30. PMID: 41347810 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
BMC Bioinformatics
Drug mechanism enrichment analysis improves prioritization of therapeutics for repurposing. [Abstract]2023 May 24;24(1):215. PMID: 37226094 -
Mol Pharmacol
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]2022 Jun;101(6):381-389. PMID: 35383108 -
PLoS One
Validated LC-MS/MS assay for quantification of the newly approved tyrosine kinase inhibitor, dacomitinib, and application to investigating its metabolic stability. [Abstract]2019 Apr 4;14(4):e0214598. PMID: 30947315 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
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Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
Solvant et solubilité
DMF : 10 mg/mL (20.49 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMF | 1 mM | 2.0494 mL | 10.2470 mL | 20.4939 mL | 51.2348 mL |
| 5 mM | 0.4099 mL | 2.0494 mL | 4.0988 mL | 10.2470 mL | |
| 10 mM | 0.2049 mL | 1.0247 mL | 2.0494 mL | 5.1235 mL | |
| 15 mM | 0.1366 mL | 0.6831 mL | 1.3663 mL | 3.4157 mL | |
| 20 mM | 0.1025 mL | 0.5123 mL | 1.0247 mL | 2.5617 mL |
Dacomitinib hydrate Related Classifications
HY-118263 Related Classifications
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