Art. -Nr.: HY-13272

Dacomitinib

(Synonyms: PF-00299804; PF-299804)

29 Cited Publications

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Based on 29 publication(s) in Google Scholar

Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

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Reinheit: 99.74%
CAS. Nr.: 1110813-31-4
Formel: C₂₄H₂₅ClFN₅O₂
Molecular Weight:469.94

Speicherung:

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

Dacomitinib Chemical Structure

CAS. Nr.: 1110813-31-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (29)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR

6 nM (IC₅₀)

ErbB2

45.7 nM (IC₅₀)

ErbB4

73.7 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

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

Dacomitinib (PF00299804) effectively inhibits the in vitro kinase activity of wild-type EGFR (IC50=6 nM)with similar efficacy. Dacomitinib also effectively inhibits wild-type ERBB2 with IC₅₀ of 45.7 nM. In H441, an IC₅₀ is reached with Dacomitinib but only at a very high concentration (4 μM) and likely reflects off-target effects. In cell lines wild-type for both EGFR and K-ras (H322, H1819, and Calu-3), ZD1839 and Dacomitinib both effectively inhibit growth of H1819 and Calu-3 cells but not of H322 cells. Dacomitinib is a pan-ERBB inhibitor and most EGFR mutant cell lines express multiple ERBB family members, the effects on EGFR phosphorylation could potentially be indirect. Dacomitinib inhibits EGFR phosphorylation in all of the different EGFR T790M proteins whereas ZD1839 is ineffective even at 10 μM. In the NIH3T3 cells, phosphorylation of EGFR L858R/T790M is completely inhibited by 1 nM Dacomitinib, whereas 100 nM or greater is required to inhibit EGFR WT/T790M or Del/T790M^[1]. The HER2-amplified cell lines are most sensitive to growth inhibition by Dacomitinib (IC₅₀<1 μM in 14 of 16 lines; 87.5%) as compared with 5 of 28 (17.9%) of HER2-nonamplified lines (excluding immortalized lines)^[2].

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

In Vivo

To evaluate the efficacy of Dacomitinib, xenografts in nu/nu mice are generated using HCC827 GFP and HCC827 Del/T790M cells and treated the mice with Dacomitinib. Dacomitinib (10 mg/kg/d by daily oral gavage) effectively inhibits the growth of HCC827 GFP xenografts. In contrast, HCC827 Del/T790M xenografts are resistant to ZD1839, whereas Dacomitinib treatment is substantially more effective at inhibiting growth of this xenograft model^[1].

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

Chemical Information

CAS. Nr. 1110813-31-4
Appearance Solid
Molecular Weight 469.94
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (29)

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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
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
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.

Lösungsmittel & Löslichkeit

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC/saline water

Solubility: 5 mg/mL (10.64 mM); Suspended solution; Need ultrasonic

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.

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 + +
%
Saline +

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

Protokoll

Cell Assay^[2]

Cells are seeded in duplicate at 5×10³ to 5×10⁴ cells per well in 24-well plates, and growth inhibition data is calculated. Briefly, day after plating, Dacomitinib is added at 10 μM and 2-fold dilutions over 12 concentrations are carried out to generate a dose-response curve. Control wells without the drug are also seeded. The cells are counted on day 1 when the drug is added, as well as after 6 days when the experiment ended. After the trypsinization cells are placed in an Isotone solution and immediately counted using a Coulter Z1 particle counter. The suspension cultures are counted using a Coulter Vi-Cell counter^[2].

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

Animal Administration^[1]

Mice^[1]
Nude mice (nu/nu; 6-8 weeks old) are used for in vivo studies. A suspension of 5×10⁶ HCC827-GFP or HCC827-Del/T790M lung cancer cells (in 0.2 mL of PBS) are inoculated s.c. into the lower-right quadrant of the flank of each mouse. Five mice are inoculated with either HCC827-GFP or HCC827-Del/T790M cells in the ZD1839 treatment group. Tumors are measured twice weekly using calipers, and volume is calculated using the following formula: length×width²×0.52. Mice are monitored daily for body weight and general condition. Mice are randomized to treatment when the mean tumor volume is 400 to 500 mm³. ZD1839 is administered at 150 mg/kg/d by daily oral gavage. Dacomitinib is administered at 10 mg/kg/d by daily oral gavage. The experiment is terminated when the mean size of the control tumors reached 2000 mm³.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
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)
Handling Instructions (2659 KB)

Verweise

[1]. Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67(24):11924-32. [Content Brief]

[2]. Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11(9):1978-87. [Content Brief]

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

Keywords

Dacomitinib

29 Cited Publications

100 mg Angebot einholen

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Dacomitinib

Apoptosis Compound Library

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Publications Citing Use of MedChemExpress (MCE) Dacomitinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (29)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dacomitinib Related Classifications

HY-13272 Related Classifications