Dacomitinib | PF-00299804;PF-299804;PF299 | Apoptosis Inducer | Tyrosine / EGF Receptor Protein Kinase Inhibitor | EGFR | HER2 | ErbB

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产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						95%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						98%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						99%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		99%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					PARP,Caspase	99%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						95%
(S)-Sunvozertinib	✔						99%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			95%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms/CSF1R	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			98%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib 2HCl	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			97%
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	99%
Brigatinib					+ EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM	ALK,FLT3	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		99%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	HER2 ↓ ↑	其他靶点	纯度
Poziotinib	++++ HER2, IC50: 5.3 nM		98%
Tyrphostin AG 879	+ HER2-Neu, IC50: 1.0 μM		95%
TAK-285	+ HER2, IC50: 17 nM		99%+
ARRY-380 analog	✔		99%
Canertinib	+++ ErbB2, IC50: 9.0 nM	EGFR	99%+
(E/Z)-CP-724714	++ HER2/ErbB2, IC50: 10 nM		95%
Lapatinib	+++ ErbB2, IC50: 9.2 nM	EGFR	98%
AEE788	++++ HER2/ErbB2, IC50: 6 nM	EGFR	98+%
Neratinib	+ HER2, IC50: 59 nM	Src,EGFR	98%
BMS-599626	+ HER2, IC50: 30 nM		98%
Mubritinib	++++ HER2/ErbB2, IC50: 6.0 nM		99%+
Tucatinib	+++ ErbB2, IC50: 8 nM		98%
Sapitinib	++++ ErbB2, IC50: 3 nM	EGFR	99%+
CUDC-101	++ HER2, IC50: 15.7 nM	EGFR,HDAC	99%+
Afatinib dimaleate	++ HER2, IC50: 14 nM		98%
Afatinib	++ HER2, IC50: 14 nM		99%
Pertuzumab	✔		95%
Trastuzumab	✔		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

靶点	EGFR/ErbB1 EGFR, IC50:6.0 nM HER2/ErbB2 ErbB2, IC50:45.7 nM ErbB4 ErbB4, IC50:73.7 nM
描述	EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1 - 4) with an external domain that binds activating ligands, such as EGF, and is overexpressed in a significant percentage of carcinomas and contributes to the malignant phenotype. Upon activation, EGFR phosphorylates both the receptor itself and a variety of “effector” protein. Dacomitinib is an irreversible pan-ERBB inhibitor with IC50 values of 6 nM，45.7 nM and 73.3 nM for EGFR, ERBB2 and ERBB4 (performed by in vitro kinase assays), respectively. Dacomitinib at concentration of 1 μM led to complete inhibition of EGFR, ERBB3 and Akt phosphorylation, as well as substantial apoptosis, in EGFR T790M–containing H3255 GR cell line. Dacomitinib inhibited both wild-type and mutant ERBB2, but showed more effective on mutant EGFR than gefitinib at similar concentrations. Dacomitinib was highly effective in a xenograft (HCC827 Del/T790M) model of T790M-mediated acquired resistance to gefitinib at dose of 10 mg/kg/d by daily oral gavage^[1].
作用机制	Dacomitinib can bind with the ATP site and make a covalent modification of nucleophilic cysteine residues in the catalytic domains of ERBB^[2].

Cell Line HUVEC HEK293/pcDNA3.1 cells S1-MI-80 cells H460/MX20 cells 22Rv1 C4-2 LNCaP GBM6 cells 452.Luc2 cells Daoy.Luc2 cells U87vIII.Luc2 cells U87.Luc2 cells WZ4002-resistant PC9 cells PC9 cells SBA-16 cells SBA-6 cells	Concentration	Treated Time	Description	References
HUVEC	2.5 μM	6 days	inhibited EGFR phosphorylation and significantly suppressed MES-GSC EV-stimulated endothelial cell migration and aortic ring outgrowth	Nat Commun. 2024 Apr 3;15(1):2865
HEK293/pcDNA3.1 cells	0.25, 0.5, 1 μM	72 h	No significant difference in the IC50 values for MX	J Exp Clin Cancer Res. 2018 Feb 20;37(1):31
S1-MI-80 cells	0.25, 0.5, 1 μM	72 h	Potentiate the anticancer activity of ABCG2 substrate anticancer drugs (MX and topotecan)	J Exp Clin Cancer Res. 2018 Feb 20;37(1):31
H460/MX20 cells	0.25, 0.5, 1 μM	72 h	Potentiate the anticancer activity of ABCG2 substrate anticancer drugs (MX and topotecan)	J Exp Clin Cancer Res. 2018 Feb 20;37(1):31
22Rv1	2 µM	72 h	To evaluate the effect of Dacomitinib on castration-resistant prostate cancer cells. Results showed that Dacomitinib reduced cell viability by 87.6% and induced apoptosis in 22Rv1 cells.	Br J Cancer. 2019 Jul;121(3):237-248
C4-2	2 µM	72 h	To evaluate the effect of Dacomitinib on castration-resistant prostate cancer cells. Results showed that Dacomitinib inhibited cell viability by 89.8% and induced apoptosis in C4-2 cells.	Br J Cancer. 2019 Jul;121(3):237-248
LNCaP	2 µM	72 h	To evaluate the effect of Dacomitinib on hormone-sensitive prostate cancer cells. Results showed that Dacomitinib reduced cell viability by 54.4% in LNCaP cells.	Br J Cancer. 2019 Jul;121(3):237-248
GBM6 cells	500 nM	Overnight	Inhibited EGFR phosphorylation and reduced phosphorylation of downstream AKT and ERK1/2	Neoplasia. 2018 May;20(5):432-442
452.Luc2 cells	6.25-400 nM	30 min	Inhibited EGFR phosphorylation and reduced phosphorylation of downstream AKT and ERK1/2	Neoplasia. 2018 May;20(5):432-442
Daoy.Luc2 cells	6.25-400 nM	30 min	Inhibited EGFR phosphorylation and reduced phosphorylation of downstream AKT and ERK1/2	Neoplasia. 2018 May;20(5):432-442
U87vIII.Luc2 cells	0.4-4 μM	30 min	Inhibited EGFRvIII phosphorylation and reduced phosphorylation of downstream AKT and ERK1/2	Neoplasia. 2018 May;20(5):432-442
U87.Luc2 cells	0.4-4 μM	30 min	Inhibited EGFRvIII phosphorylation and reduced phosphorylation of downstream AKT and ERK1/2	Neoplasia. 2018 May;20(5):432-442
WZ4002-resistant PC9 cells	1 μM	72 h	Evaluate the growth inhibitory effect of WZ4002 on PC9 cells and their resistant clones, showing that the IC50 of resistant cells to WZ4002 was about 10-fold higher than that of parental PC9 cells	Cancer Res. 2013 Jan 15;73(2):834-43.
PC9 cells	1 μM	72 h	Evaluate the growth inhibitory effect of PF299804 on PC9 cells and their resistant clones, showing that the IC50 of resistant cells to PF299804 was more than 100-fold higher than that of parental PC9 cells	Cancer Res. 2013 Jan 15;73(2):834-43.
SBA-16 cells	2.5nM	72 h	To evaluate the anti-proliferative effect of Dacomitinib on ERBB2-mutant cell lines, showing an IC50 of 2.5nM.	Clin Cancer Res. 2019 Jan 15;25(2):641-651
SBA-6 cells	1nM	72 h	To evaluate the anti-proliferative effect of Dacomitinib on ERBB2-mutant cell lines, showing an IC50 of 1nM.	Clin Cancer Res. 2019 Jan 15;25(2):641-651

Species NSG mice Nude mice (BALB/c-nu/nu) Mice Nude mice	Animal Model Glioblastoma xenograft model H460/MX20 cell xenograft model U87vIII.Luc2 glioblastoma xenograft model PDX6 and PDX16 models	Administration	Dosage	Frequency	Description	References
NSG mice	Glioblastoma xenograft model	Oral gavage	15 mg/kg	5 consecutive days followed by a 2-day break	Evaluated the effect of Dacomitinib alone or in combination with anti-VEGFR2 antibody on tumor growth and vascular patterns, significantly prolonged survival and disrupted vasectasia	Nat Commun. 2024 Apr 3;15(1):2865
Nude mice (BALB/c-nu/nu)	H460/MX20 cell xenograft model	Oral	5 mg/kg	Every other day for 25 days	Significantly enhanced the antitumor efficacy of topotecan in ABCG2-overexpressing H460/MX20 cell xenografts	J Exp Clin Cancer Res. 2018 Feb 20;37(1):31
Mice	U87vIII.Luc2 glioblastoma xenograft model	Oral gavage	30 mg/kg	Thrice weekly	Dacomitinib significantly extended the lifespan of mice bearing U87vIII.Luc2 glioblastoma xenografts	Neoplasia. 2018 May;20(5):432-442
Nude mice	PDX6 and PDX16 models	Oral	10mg/kg	Once daily for 3 weeks	To evaluate the inhibitory effect of Dacomitinib on ERBB2-mutant tumors, showing tumor growth reduction by 39% and 59% in PDX6 and PDX16, respectively.	Clin Cancer Res. 2019 Jan 15;25(2):641-651

CAS号	1110813-31-4
分子式	C₂₄H₂₅ClFN₅O₂
分子量	469.94
SMILES Code	O=C(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OC)/C=C/CN4CCCCC4
MDL No.	MFCD19443734

别名	PF-00299804; PF-299804; PF299
运输	蓝冰
InChI Key	LVXJQMNHJWSHET-AATRIKPKSA-N
Pubchem ID	11511120

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EGFR/ErbB1	EGFR, IC50:6.0 nM
HER2/ErbB2	ErbB2, IC50:45.7 nM
ErbB4	ErbB4, IC50:73.7 nM

human LoVo cells	Function assay	2 h	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay, IC50=0.011 μM	23930994
human NCI-H1975 cells	Function assay	2 h	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50=0.042 μM	23930994
human NCI-H1975 cells	Proliferation assay		Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition, GI50=0.1233 μM	26310890
PC9 cells	Function assay	2 h	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50=0.63 nM	23930994

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