Cat. No.: HY-13272

Dacomitinib

Name: Dacomitinib
Brand: MedChemExpress
SKU: HY-13272
Price: 92.00 USD
Availability: InStock
Rating: 5 (31 reviews)

(Synonyms: PF-00299804; PF-299804)

31 Cited Publications

고객리뷰

Based on 31 publication(s) in Google Scholar

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.

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Purity : 99.74%
CAS No.: 1110813-31-4
화학식: C₂₄H₂₅ClFN₅O₂
분자량:469.94

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Dacomitinib Chemical Structure

CAS No.: 1110813-31-4

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (31)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
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Bioz

Biological Activity

제품 설명

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)

All EGFR Isoforms :

All IAP Isoforms :

All Akt Isoforms :

All ERK Isoforms :

All PI3K Isoforms :

All Caspase Isoforms :

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	6 nM Compound: 2	Antiproliferative activity against human A-431 cells harboring EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay Antiproliferative activity against human A-431 cells harboring EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay	[PMID: 37499291]
A-431	IC₅₀	1.96 μM Compound: Dacomitinib	Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
A549	IC₅₀	>10 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human A549 cells harboring K-ras G12S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human A549 cells harboring K-ras G12S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
A549	IC₅₀	0.49 μM Compound: Dacomitinib	Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
BaF3	IC₅₀	<1 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.2 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.4 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.6 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.9 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	140 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	160 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	2 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	2.6 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	230 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR A767_V769duspASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR A767_V769duspASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	240 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	270 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	300 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	330 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BT-474	IC₅₀	18 nM Compound: Dacomitinib	Antiproliferative activity against human BT-474 cells Antiproliferative activity against human BT-474 cells	[PMID: 33429247]
Calu-3	IC₅₀	0.063 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human Calu-3 cells overexpressing ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Calu-3 cells overexpressing ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
H322	IC₅₀	>10 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human H322 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human H322 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC4006	IC₅₀	0.004 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC4006 cells harboring EGFR Del L747_E749 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC4006 cells harboring EGFR Del L747_E749 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.003 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.014 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.061 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.083 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 Ins 774YVMA assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 Ins 774YVMA assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	GI₅₀	5 nM Compound: 2	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay	[PMID: 37499291]
HCC827	IC₅₀	0.007 μM Compound: Dacomitinib	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
HEK293	IC₅₀	0.185 μM Compound: Dacomitinib	Cytotoxicity against HEK293 cells expressing ABCG2 in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2 in presence of methotrexate	[PMID: 35944339]
LoVo	IC₅₀	0.011 μM Compound: 5	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	IC₅₀	0.44 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H1975	IC₅₀	0.042 μM Compound: 5	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	IC₅₀	0.042 μM Compound: 5	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	GI₅₀	123.3 nM Compound: Dacomitinib	Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition	[PMID: 26310890]
NCI-H1975	IC₅₀	0.44 μM Compound: 32; PF00299804	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H1975	IC₅₀	0.7 μM Compound: Dacomitinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
NCI-H3255	IC₅₀	0.007 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	0.007 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	0.137 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	1.57 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	1.62 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H441	IC₅₀	4 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H441 cells harboring K-ras G12V mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H441 cells harboring K-ras G12V mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
PC-9	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
PC-9	IC₅₀	0.00063 μM Compound: 5	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
PC-9	IC₅₀	0.63 nM Compound: 5	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
Sf9	IC₅₀	0.006 μM Compound: 54; PF-00299804	Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	0.046 μM Compound: 54; PF-00299804	Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	0.074 μM Compound: 54; PF-00299804	Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	3.57 μM Compound: 54; PF-00299804	Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA	[PMID: 27491023]
SK-BR-3	IC₅₀	15 nM Compound: Dacomitinib	Antiproliferative activity against human SK-BR-3 cells Antiproliferative activity against human SK-BR-3 cells	[PMID: 33429247]

In Vitro

Anti-cancerApoptosisCell Cycle RegulationAutophagyOthers

Anti-cancer

Dacomitinib (5 μM; 48 h) 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) 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) 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) inhibits the phosphorylation of EGFR, ERK, and Akt in UM-UC cells, indicating receptor target-driven signaling inhibition^[2].
Dacomitinib 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) 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) 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) 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) 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 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) 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) 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) 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) 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 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) induces G1 cell cycle arrest in UM-UC-6 and UM-UC-9 bladder cancer cells^[2].
Dacomitinib (50 nM; 24 h) attenuates hypoxia-induced cell cycle progression in primary rat PASMCs by reducing the S-phase cell population^[7].

Others

Dacomitinib 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) 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) 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.

Cell Proliferation Assay^[1]

Cell Line:

AsPC-1, PANC-1, and PaTu 8902
Concentration:

5 μM
Incubation Time:

48 h
Result:

Inhibited the proliferation of AsPC-1, PANC-1, and PaTu 8902 PDAC cells, it enhanced the radiosensitivity of the cells by inhibiting growth.

Cell Viability Assay^[1]

Cell Line:

AsPC-1, PANC-1, and PaTu 8902
Concentration:

5 μM
Incubation Time:

48 h
Result:

Diminished cell density in AsPC-1, PANC-1, and PaTu 8902 cellsl, it enhanced the radiosensitivity of the cells by inhibiting growth.

Apoptosis Analysis^[1]

Cell Line:

AsPC-1, PANC-1, and PaTu 8902
Concentration:

5 μM
Incubation Time:

48 h
Result:

Induced apoptosis in AsPC-1, PANC-1, and PaTu 8902 PDAC cells; when combined with 2 Gy γ-ray, it enhanced the radiosensitivity of the cells by inducing apoptosis.

Cell Migration Assay ^[1]

Cell Line:

AsPC-1, PANC-1, and PaTu 8902
Concentration:

5 μM
Incubation Time:

48 h
Result:

Inhibited the migration and invasion of AsPC-1, PANC-1, and PaTu 8902 PDAC cells.

Cell Viability Assay^[2]

Cell Line:

UM-UC-6, UM-UC-9
Concentration:

2 μmol/L
Incubation Time:

72 h
Result:

Reduced cell viability significantly in UM-UC-6 and UM-UC-9 cell lines.

Cell Cycle Analysis^[2]

Cell Line:

UM-UC-6, UM-UC-9
Concentration:

2 μmol/L
Incubation Time:

24, 30, or 44 h
Result:

Induced G1 cell cycle arrest in UM-UC-6 and UM-UC-9 bladder cancer cells.

Apoptosis Analysis^[2]

Cell Line:

UM-UC-6, UM-UC-9
Concentration:

2 μmol/L
Incubation Time:

48 h
Result:

Induced apoptosis in UM-UC-6 cells but not in UM-UC-9 cells, while increasing necrosis in both cell lines.

Western Blot Analysis^[5]

Cell Line:

human breast cancer cell lines with variable HER receptor levels
Concentration:

0.1, 1 μmol/L
Incubation Time:

10 minutes
Result:

Inhibited phosphorylation of HER2, EGFR, HER4, AKT, and ERK in sensitive HER2-amplified breast cancer cell lines.

Cell Cycle Analysis^[5]

Cell Line:

BT-474, SK-BR-3, MCF-7, ZR-75-1, HCC-1143, MDA-MB-231
Concentration:

100 nmol/L-1 μmol/L
Incubation Time:

48 hours; 5 days
Result:

Induced significant G0-G1 cell-cycle arrest in BT-474 and SK-BR-3 lines and less pronounced yet statistically significant G0-G1 arrest in MCF-7.
Caused no changes in cell cycle in ZR-75-1, HCC-1143, and MDA-MB-231 lines.
Showed no difference in cell cycle between 48-hour and 5-day treatment time points in BT-474 and SK-BR-3 lines.

Apoptosis Analysis^[5]

Cell Line:

BT-474, SK-BR-3, HCC-1143, ZR-75-1, MDA-MB-231
Concentration:

1 μmol/L
Incubation Time:

5 days
Result:

Induced a significant increase in apoptosis in BT-474, SK-BR-3, and HCC-1143 lines.
Induced no changes in resistant lines.

Apoptosis Analysis^[5]

Cell Line:

BT-474, SK-BR-3
Concentration:

100 nmol/L, 1 μmol/L
Incubation Time:

48 hours, 5 days
Result:

Showed no difference in cell cycle between 48-hour and 5-day time points.
Induced no apoptosis in SK-BR-3 at 48 hours.
Induced apoptosis in BT-474 at 48 hours, albeit at lesser degree than at 5 days.

Cell Cycle Analysis^[5]

Cell Line:

BT-474-TR, SK-BR-3-TR, BT-474-LR, SK-BR-3-LR
Concentration:

100 nmol/L, 1 μmol/L
Incubation Time:

48 hours, 5 days
Result:

Caused a G0-G1 arrest comparable with parental lines in trastuzumab-resistant lines.
Caused a G0-G1 arrest similar to parental lines at 1 μmol/L in lapatinib-resistant lines.
Showed a less pronounced effect at 100 nmol/L in lapatinib-resistant lines.

Apoptosis Analysis^[5]

Cell Line:

BT-474-TR, SK-BR-3-TR, BT-474-LR, SK-BR-3-LR
Concentration:

100 nmol/L-1 μmol/L
Incubation Time:

5 days
Result:

Induced stronger apoptosis in trastuzumab-resistant lines than in parental lines.
Did not induce apoptosis at 100 nmol/L in lapatinib-resistant lines.
Showed a less pronounced effect at 1 μmol/L in lapatinib-resistant lines than in parental lines.

Cell Proliferation Assay^[7]

Cell Line:

Primary rat pulmonary artery smooth muscle cells (PASMCs)
Concentration:

50 nM
Incubation Time:

24 h
Result:

Inhibited PASMCs proliferation under both normoxia and hypoxia conditions.
Inhibited EGF- and hypoxia-induced proliferation.

Cell Migration Assay ^[7]

Cell Line:

Primary rat pulmonary artery smooth muscle cells (PASMCs)
Concentration:

50 nM
Incubation Time:

24 h
Result:

Significantly inhibited hypoxia-induced migration of PASMCs.

Cell Cycle Analysis^[7]

Cell Line:

Primary rat pulmonary artery smooth muscle cells (PASMCs)
Concentration:

50 nM
Incubation Time:

24 h
Result:

Attenuated hypoxia-induced changes in cell cycle distribution, reducing the percentage of cells in S phase and increasing cells at G0/G1 phase.

Western Blot Analysis^[7]

Cell Line:

Primary rat pulmonary artery smooth muscle cells (PASMCs)
Concentration:

50 nM
Incubation Time:

24 h
Result:

Reduced cyclin A, cyclin D, CDK1, and CDK2 protein levels in primary rat PASMCs.

Immunofluorescence^[7]

Cell Line:

Primary rat pulmonary artery smooth muscle cells (PASMCs)
Concentration:

50 nM
Incubation Time:

24 h
Result:

Inhibited the appearance of eGFP-mRFP-LC3 adenoviruses under hypoxia.

Cell Viability Assay^[8]

Cell Line:

T84
Concentration:

1, 2, 4 μM
Incubation Time:

0, 24, 48 h
Result:

Showed no significant differences.

In Vivo

Anti-cancerCardiovascular RegulationRegulation of Cardiac Pump FunctionOthers

Anti-cancer

Dacomitinib (6 mg/kg; oral; once daily; 4 wks (early); 3 wks (advanced)) 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) 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) 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) 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) 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.

Animal Model:

NOD/SCID mice (six-month-old, male)^[2]
Dosage:

6 mg/kg
Administration:

p.o.; once daily; starting 1 d (early) or 1 wk (late) after cell inoculation, treatment duration was 4 and 3 wks, respectively
Result:

Inhibited the growth of UM-UC-6 bladder cancer xenografts, accompanied by target-specific pharmacodynamic changes, including inhibition of EGFR and ERK phosphorylation and decreased E-cadherin expression; and it inhibits the growth of UM-UC-9 bladder cancer xenografts.

Animal Model:

Sprague-Dawley (adult male, 6 weeks old, approximately 200 g)^[7]
Dosage:

100, 250, 500 nmol/kg/day
Administration:

s.c.; daily; starting 2 weeks after monocrotaline injection for 3 weeks
Result:

Attenuated MCT-induced pulmonary vascular remodeling and pulmonary hypertension in rats.

Related Protocols :

Chemical Information

CAS No. 1110813-31-4
Appearance Solid
분자량 469.94
화학식 C₂₄H₂₅ClFN₅O₂
Color White to yellow
SMILES

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

PF-00299804; PF-299804
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (31)

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

Sort by:

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 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 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 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 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 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.

용액&용해도

In Vitro:

DMSO : 38.89 mg/mL (82.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1279 mL

10.6397 mL

21.2793 mL

5 mM

0.4256 mL

2.1279 mL

4.2559 mL

10 mM

0.2128 mL

1.0640 mL

2.1279 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.32 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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μL
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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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (308 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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OR (2659 KB)
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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.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1279 mL	10.6397 mL	21.2793 mL	53.1983 mL
	5 mM	0.4256 mL	2.1279 mL	4.2559 mL	10.6397 mL
	10 mM	0.2128 mL	1.0640 mL	2.1279 mL	5.3198 mL
	15 mM	0.1419 mL	0.7093 mL	1.4186 mL	3.5466 mL
	20 mM	0.1064 mL	0.5320 mL	1.0640 mL	2.6599 mL
	25 mM	0.0851 mL	0.4256 mL	0.8512 mL	2.1279 mL
	30 mM	0.0709 mL	0.3547 mL	0.7093 mL	1.7733 mL
	40 mM	0.0532 mL	0.2660 mL	0.5320 mL	1.3300 mL
	50 mM	0.0426 mL	0.2128 mL	0.4256 mL	1.0640 mL
	60 mM	0.0355 mL	0.1773 mL	0.3547 mL	0.8866 mL
	80 mM	0.0266 mL	0.1330 mL	0.2660 mL	0.6650 mL

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Dacomitinib

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Dacomitinib

Publications Citing Use of MedChemExpress (MCE) Dacomitinib

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Publications (31)

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In Vivo Dissolution Calculator

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Dacomitinib

Publications Citing Use of MedChemExpress (MCE) Dacomitinib

All EGFR Isoforms

All IAP Isoforms

All Akt Isoforms

All ERK Isoforms

All PI3K Isoforms

All Caspase Isoforms

All CDK Isoforms

Biological Activity

제품 설명

IC50 & Target

Cellular Effect

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Publications (31)

용액&용해도

In Vitro:

In Vivo:

In Vivo Dissolution Calculator

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References

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Complete Stock Solution Preparation Table

Dacomitinib Related Classifications

HY-13272 Related Classifications

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