Cat. No.: HY-118263

Dacomitinib hydrate

Name: Dacomitinib hydrate
Brand: MedChemExpress
SKU: HY-118263
Price: 90.00 USD
Availability: InStock
Rating: 5 (31 reviews)

(Synonyms: PF-00299804 hydrate; PF-299804 hydrate)

31 Cited Publications

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Based on 31 publication(s) in Google Scholar

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.

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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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Dacomitinib hydrate Chemical Structure

CAS No.: 1042385-75-0

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

HY-112870A
Firmonertinib mesylate

EGFR Inhibitor

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (31)
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Activité biologique

Description

IC₅₀ & Target

^[7]^[2]^[4]

CDK1

CDK2

Caspase-3

Caspase-7

Akt

ERK

EGFR

HER1

6 nM (IC₅₀)

HER2

45.7 nM (IC₅₀)

HER4

73.7 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

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Cellular Effect

Cell Line	Type	Value	Description	References
HCC1419	IC50	0.006 μM	Antiproliferative activity against human HCC-1419 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1419 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MCF-10A	IC50	0.008 μM	Antiproliferative activity against human MCF-10A breast epithelial cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MCF-10A breast epithelial cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
SK-BR-3	IC50	0.015 μM	Antiproliferative activity against human SK-BR-3 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human SK-BR-3 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
UACC-893	IC50	0.017 μM	Antiproliferative activity against human UACC-893 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human UACC-893 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
BT-474	IC50	0.018 μM	Antiproliferative activity against human BT-474 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human BT-474 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-361	IC50	0.03 μM	Antiproliferative activity against human MDA-MB-361 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-361 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
UACC-812	IC50	0.04 μM	Antiproliferative activity against human UACC-812 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human UACC-812 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1954	IC50	0.06 μM	Antiproliferative activity against human HCC-1954 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1954 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
184B5	IC50	0.08 μM	Antiproliferative activity against human 184B5 breast epithelial cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human 184B5 breast epithelial cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
ZR-75-1	IC50	0.24 μM	Antiproliferative activity against human ZR-75-1 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human ZR-75-1 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-415	IC50	0.67 μM	Antiproliferative activity against human MDA-MB-415 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-415 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1143	IC50	0.73 μM	Antiproliferative activity against human HCC-1143 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1143 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1569	IC50	0.77 μM	Antiproliferative activity against human HCC-1569 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1569 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
EFM-19	IC50	1.07 μM	Antiproliferative activity against human EFM-19 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human EFM-19 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
COLO-824	IC50	1.20 μM	Antiproliferative activity against human COLO-824 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human COLO-824 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-157	IC50	1.36 μM	Antiproliferative activity against human MDA-MB-157 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-157 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
T47D	IC50	1.41 μM	Antiproliferative activity against human T-47D breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human T-47D breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-468	IC50	1.42 μM	Antiproliferative activity against human MDA-MB-468 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-468 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC70	IC50	1.44 μM	Antiproliferative activity against human HCC-70 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-70 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1187	IC50	1.46 μM	Antiproliferative activity against human HCC-1187 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1187 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-134-VI	IC50	1.74 μM	Antiproliferative activity against human MDA-MB-134 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-134 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1395	IC50	1.77 μM	Antiproliferative activity against human HCC-1395 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1395 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-453	IC50	2.00 μM	Antiproliferative activity against human MDA-MB-453 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-453 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1937	IC50	2.04 μM	Antiproliferative activity against human HCC-1937 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1937 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC1806	IC50	2.05 μM	Antiproliferative activity against human HCC-1806 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-1806 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
BT-549	IC50	2.22 μM	Antiproliferative activity against human BT-549 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human BT-549 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
HCC38	IC50	2.40 μM	Antiproliferative activity against human HCC-38 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human HCC-38 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-436	IC50	2.56 μM	Antiproliferative activity against human MDA-MB-436 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-436 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
BT-20	IC50	2.58 μM	Antiproliferative activity against human BT-20 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human BT-20 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
CAMA-1	IC50	2.68 μM	Antiproliferative activity against human CAMA-1 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human CAMA-1 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
CAL-51	IC50	2.76 μM	Antiproliferative activity against human CAL-51 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human CAL-51 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-435	IC50	2.92 μM	Antiproliferative activity against human MDA-MB-435 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-435 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
Hs-578T	IC50	2.92 μM	Antiproliferative activity against human Hs578T breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human Hs578T breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
DU-4475	IC50	3.55 μM	Antiproliferative activity against human DU-4475 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human DU-4475 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MCF7	IC50	3.67 μM	Antiproliferative activity against human MCF-7 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MCF-7 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403
MDA-MB-231	IC50	4.23 μM	Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter. Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as growth inhibition after 6 days by Coulter counter.	22761403

In Vitro

Anti-cancerApoptosisCell Cycle RegulationAutophagyOthers

Anti-cancer

Dacomitinib (5 μM; 48 h) hydrate significantly inhibits the proliferation and reduces the viability of AsPC-1, PANC-1, and PaTu 8902 PDAC cells; when combined with 2 Gy γ-irradiation, it enhances the radiosensitivity of the cells by inhibiting growth^[1].
Dacomitinib (5 μM; 48 h) hydrate inhibits the migration and invasion of AsPC-1, PANC-1, and PaTu 8902 PDAC cells^[1].
Dacomitinib (Dac) (1 nmol/L-2 μmol/L; 72 h) hydrate is effective against bladder cancer cells expressing multiple HER family target receptors, among which UM-UC-6 and UM-UC-9 cells are more sensitive than UM-UC-3 cells^[2].
Dacomitinib (0.02-2 μmol/L; 5 h) hydrate inhibits the phosphorylation of EGFR, ERK, and Akt in UM-UC cells, indicating receptor target-driven signaling inhibition^[2].
Dacomitinib hydrate preferentially inhibits the proliferation of HER2-amplified breast cancer cell lines, with IC₅₀ values below 1 μmol/L in the vast majority of HER2-amplified cell lines^[5].
Dacomitinib (0.1-1 μmol/L; 10 minutes) hydrate inhibits the phosphorylation of HER2, EGFR, HER4, AKT, and ERK in sensitive HER2-amplified breast cancer cell lines^[5].
Dacomitinib (1-4 μM; 24-48 h) hydrate does not alter TEER or cell viability in T84 colorectal cancer cells, indicating that it does not cause direct cytotoxicity^[8].

Anti-cancer

Apoptosis

Dacomitinib (5 μM; 48 h) hydrate induces apoptosis in AsPC-1, PANC-1, and PaTu 8902 PDAC cells; when combined with 2 Gy γ-ray irradiation, it enhances the radiosensitivity of the cells by inducing apoptosis^[1].

Anti-cancer

Apoptosis

Cell Cycle Regulation

Dacomitinib (5 μM) hydrate modulates the expression of multiple genes and proteins in AsPC-1, PANC-1, and PaTu 8902 PDAC cells; it downregulates the epithelial-mesenchymal transition-related proteins ZEB1, N-cadherin, and Snail as well as the anti-apoptotic proteins cIAP2, cIAP1, XIAP, MCL1, and survivin, reduces the mRNA levels of FOXM1, PLK1, Aurora kinase B, cyclin D1, c-Myc, the anti-apoptotic genes survivin, XIAP, cIAP1, cIAP2, and MCL1, and the metastasis-related genes MMP2, CDH2, uPA, uPAR, and CSTB, while upregulating the mRNA expression of the pro-apoptotic genes PUMA and BAX and the metastasis suppressor gene CSTA^[1].
Dacomitinib hydrate overcomes acquired resistance to Trastuzumab (HY-P9907) and retains significant antiproliferative activity in Lapatinib (HY-50898)-resistant HER2-amplified breast cancer cell lines; it induces G0-G1 phase cell cycle arrest; it induces stronger apoptosis in Trastuzumab-resistant cells than in the parental cell line, shows a weaker apoptotic effect in Lapatinib-resistant cells, and simultaneously reduces the phosphorylation levels of HER2, EGFR, AKT, and ERK in both types of resistant cells^[1].
Dacomitinib (5 μM; 4-48 hours) hydrate restores the sensitivity of HRGβ-1-stimulated Caov4 cells to Cisplatin (HY-17394); in chemotherapy-resistant OVCAR3, SKOV3, and A2780CP epithelial ovarian cancer cells, it inhibits cell growth and clonogenic ability, reduces anoikis resistance, induces apoptosis, inhibits ErbB receptor activation, blocks the PLK1-FOXM1 signaling pathway and the mRNA expression of its downstream target genes, downregulates EMT marker expression, and inhibits cell migration and invasion^[1].

Anti-cancer

Cell Cycle Regulation

Dacomitinib (100 nmol/L-1 μmol/L; 48 hours-5 days) hydrate induces G0-G1 cell cycle arrest in sensitive HER2-amplified BT-474 and SK-BR-3 breast cancer cell lines^[5].

Apoptosis

Anti-cancer

Dacomitinib (2 μmol/L; 48 h) hydrate induces apoptosis in UM-UC-6 cells but not in UM-UC-9 cells, while increasing necrosis in both cell lines; moreover, it induces caspase 3/7 cleavage in UM-UC-6 cells^[2].
Dacomitinib (100 nmol/L-1 μmol/L; 48 hours-5 days) hydrate induces apoptosis in sensitive HER2-amplified BT-474 and SK-BR-3 breast cancer cell lines; more than 48 hours is required to induce apoptosis in SK-BR-3, whereas BT-474 shows earlier induction at 48 hours^[5].

Autophagy

Cell Cycle Regulation

Dacomitinib hydrate decreases the protein levels of cyclin A, cyclin D, CDK1, and CDK2 in primary rat PASMCs; in primary rat PASMCs under hypoxic conditions, it promotes protective autophagy (with altered expression of LC3B‑II, BECN‑1, and SQSTM‑1), inhibits the PI3K‑AKT‑mTOR signaling pathway by downregulating phosphorylation at Akt (Ser 473) and mTOR (Ser 248) sites; it also inhibits eGFP‑mRFP‑LC3 adenovirus‑related signaling^[1].

Cell Cycle Regulation

Dacomitinib (2 μmol/L; 24-44 h) hydrate induces G1 cell cycle arrest in UM-UC-6 and UM-UC-9 bladder cancer cells^[2].
Dacomitinib (50 nM; 24 h) hydrate attenuates hypoxia-induced cell cycle progression in primary rat PASMCs by reducing the S-phase cell population^[7].

Others

Dacomitinib hydrate potently inhibits wild-type HER1/EGFR, HER2, and HER4 tyrosine kinases, with IC₅₀ values of 6.0, 45.7, and 73.7 nM, respectively^[4].
Dacomitinib (50 nM; 24 h) hydrate significantly inhibits the proliferation of primary rat PASMCs under both normoxic and hypoxic conditions; it significantly inhibits EGF- and hypoxia-induced proliferation of primary rat PASMCs^[7].
Dacomitinib (50 nM; 24 h) hydrate inhibits hypoxia-induced migration of primary rat PASMCs^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Anti-cancerCardiovascular RegulationRegulation of Cardiac Pump FunctionOthers

Anti-cancer

Dacomitinib (6 mg/kg; oral; once daily; 4 wks (early); 3 wks (advanced)) hydrate significantly inhibits the growth of UM-UC-6 bladder cancer xenografts, accompanied by target-specific pharmacodynamic changes, including inhibition of EGFR and ERK phosphorylation and reduced E-cadherin expression; and inhibits the growth of UM-UC-9 bladder cancer xenografts^[2].
Dacomitinib (6 mg/kg; oral; daily; 3 weeks) hydrate exhibits significant single-agent in vivo activity in a chemotherapy-resistant bladder cancer xenograft model; moreover, it is well tolerated in combination with chemotherapy and significantly enhances the effect of single-agent chemotherapy on UM-UC-9 xenograft tumors^[2].

Cardiovascular Regulation

Regulation of Cardiac Pump Function

Dacomitinib (500 nmol/kg/day; subcutaneous injection; once daily; starting 2 weeks after hypoxia induction until the terminal experiment) hydrate attenuates hypoxia-induced pulmonary vascular remodeling and pulmonary hypertension in rats^[7].
Dacomitinib (100-500 nmol/kg/day; subcutaneous injection; daily; starting 2 weeks after Monocrotaline (HY-N0750) injection for 3 weeks) hydrate attenuates MCT-induced pulmonary vascular remodeling and pulmonary arterial hypertension in rats^[7].

Others

Dacomitinib (7.5 mg/kg; oral; daily; 7 or 21 days) hydrate induces severe ileal injury, increased MCP-1 expression in the ileum, and increased gastrointestinal permeability in rats^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS No. 1042385-75-0
Appearance Solid
Masse moléculaire 487.95
Formule C₂₄H₂₇ClFN₅O₃
Color White to light yellow
SMILES

O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F.O
Synonyms

PF-00299804 hydrate; PF-299804 hydrate
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (31)

All Cell Proliferation/Viability AssayWBIn Vivo Efficacy StudyFlow CytometryCell Imaging/Staining

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Journal Impact Factor

Cancer Res

C-terminal Truncation and Fusion Partner Determine Oncogenicity of FGFR3. [Abstract]

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.
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.
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

Discovery of PLpro and Mpro Inhibitors for SARS-CoV-2. [Abstract]

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.
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
J Integr Neurosci

2026 Aug 13;25(8):51000. PMID: 42695263
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

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485
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
Biomed Pharmacother

2026 Sep:202:119803. PMID: 42537395
bioRxiv

2025 May 10.
bioRxiv

2023 Dec 12.
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841
bioRxiv

2020 Jun.

Solvant et solubilité

In Vitro:

DMF : 10 mg/mL (20.49 mM; Need ultrasonic)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0494 mL

10.2470 mL

20.4939 mL

5 mM

0.4099 mL

2.0494 mL

4.0988 mL

10 mM

0.2049 mL

1.0247 mL

2.0494 mL

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.

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Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMF 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (2.05 mM); Clear solution

Protocol 2

Add each solvent one by one: 10% DMF 90% Corn Oil

Solubility: ≥ 1 mg/mL (2.05 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

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Dacomitinib hydrate

31 Cited Publications

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Dacomitinib hydrate

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