|(E)-N-(4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)-4-(哌啶-1-基)丁-2-烯酰胺|CsnPharm

CAS No.: 1110813-31-4

达克替尼 Catalog No. CSN13899

Synonyms: PF-00299804;PF-299804;PF-299

Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:6nM ERBB4

IC50:73.7nM HER2

IC50:45.7nM
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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究

剂量

Rat^[3] (p.o.): min = 2 mg/kg, max = 500 mg/kg

给药途径

p.o.

动物药代数据

Animal	Rats^[3]	Dogs^[3]
Dose	50 mg/kg	50 mg/kg
Administration	p.o.	p.o.
C_max	630 ng/ml	870 ng/ml
T_1/2	19.4 h	21 h
F	0.8	0.74
AUC	18800 ng·h/ml	24000 ng·h/ml

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02353936	Squamous Cell Carcinoma of Eso... more >>phagus Collapse <<	Phase 2	Recruiting	January 2019	Korea, Republic of ... more >> Severance hospital Recruiting Seoul, Korea, Republic of, 120-752 Contact: Hye Ryun Kim, MD 82-2-2228-8125 nobelg@yuhs.ac Collapse <<
NCT03770988	Inoperable or Recurrent or Met... more >>astatic Esophageal Squamous Carcinoma Collapse <<	Phase 2	Not yet recruiting	August 31, 2020	Korea, Republic of ... more >> Severance Hospital Not yet recruiting Seoul, Korea, Republic of, 03722 Contact: Hye Ryun Kim, MD 82 2 2228 8125 nobleg@yuhs.ac Collapse <<
NCT01920061	Neoplasm	Phase 1	Recruiting	January 2019	-

更多
参考文献

[1] Engelman JA, Zejnullahu K, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15;67(24):11924-32.
[2] Gonzales AJ, Hook KE, et al. Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2008 Jul;7(7):1880-9.
[3] Pharmacodynamic reports of dacomitinib

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 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

技术信息

CAS号

1110813-31-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H25ClFN5O2

运输

蓝冰

分子量

469.94

别名

PF-00299804;PF-299804;PF-299;Vizimpro;达克替尼

溶解度

DMSO	50.0 mg/mL (106.4 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	45 mg/mL	suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02353936	Squamous Cell Carcinoma of Eso... more >>phagus Collapse <<	Phase 2	Recruiting	January 2019	Korea, Republic of ... more >> Severance hospital Recruiting Seoul, Korea, Republic of, 120-752 Contact: Hye Ryun Kim, MD 82-2-2228-8125 nobelg@yuhs.ac Collapse <<
NCT03770988	Inoperable or Recurrent or Met... more >>astatic Esophageal Squamous Carcinoma Collapse <<	Phase 2	Not yet recruiting	August 31, 2020	Korea, Republic of ... more >> Severance Hospital Not yet recruiting Seoul, Korea, Republic of, 03722 Contact: Hye Ryun Kim, MD 82 2 2228 8125 nobleg@yuhs.ac Collapse <<
NCT01920061	Neoplasm	Phase 1	Recruiting	January 2019	-
NCT01608022	Esophageal Squamous Cell Carci... more >>noma Collapse <<	Phase 2	Completed	-	Korea, Republic of ... more >> Severance hospital Seoul, Korea, Republic of, 120-752 Collapse <<
NCT01318031	Healthy Volunteers	Phase 1	Completed	-	United States, Connecticut ... more >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Collapse <<
NCT01313793	Healthy Volunteers	Phase 1	Completed	-	Belgium ... more >> Pfizer Investigational Site Bruxelles, Belgium, B-1070 Collapse <<
NCT01000025	Lung Cancer	Phase 3	Completed	-	-
NCT00769067	Non-small Cell Lung Cancer	Phase 2	Completed	-	-
NCT00768664	Head and Neck Neoplasms	Phase 2	Completed	-	Canada, British Columbia ... more >> Pfizer Investigational Site Vancouver, British Columbia, Canada, V5Z 4E6 Pfizer Investigational Site Vancouver, British Columbia, Canada, V5Z1H7 Canada, Ontario Pfizer Investigational Site Hamilton, Ontario, Canada, L8V 5C2 Pfizer Investigational Site London, Ontario, Canada, N6A 4L6 Pfizer Investigational Site Ottawa, Ontario, Canada, K1H 8L6 Pfizer Investigational Site Ottawa, Ontario, Canada, K1Y 4K7 Pfizer Investigational Site Toronto, Ontario, Canada, M4N 3M5 Pfizer Investigational Site Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Pfizer Investigational Site Montreal, Quebec, Canada, H2L 4M1 Collapse <<
NCT00769067	-	-	Completed	-	-
NCT01121575	Non Small Cell Lung Cancer	Phase 1	Completed	-	United States, Colorado ... more >> Clinical Trials Office University of Colorado Hospital (CTO) Aurora, Colorado, United States, 80045 DRUG SHIPMENT: University of Colorado Cancer Center Aurora, Colorado, United States, 80045 Rocky Mountain Lions Eye Institute Aurora, Colorado, United States, 80045 University of Colorado Hospital Aurora, Colorado, United States, 80045 United States, Maryland CCR, National Cancer Institute Bethesda, Maryland, United States, 20892 United States, Massachusetts Drug Shipment Only Boston, Massachusetts, United States, 02114 Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Brigham & Women's Hospital Boston, Massachusetts, United States, 02115 Drug Shipment Only Boston, Massachusetts, United States, 02215 Australia, Victoria Peter MacCallum Cancer Centre, Division of Haematology and Medical Oncology East Melbourne, Victoria, Australia, 3002 Collapse <<
NCT00783328	Neoplasms	Phase 1	Completed	-	Japan ... more >> Pfizer Investigational Site Sunto-gun, Shizuoka, Japan Collapse <<
NCT01000025	-	-	Completed	-	-
NCT00548093	Carcinoma, Non Small Cell Lung	Phase 2	Completed	-	United States, California ... more >> Pfizer Investigational Site Duarte, California, United States, 91010 Pfizer Investigational Site Pasadena, California, United States, 91105 Pfizer Investigational Site South Pasadena, California, United States, 91030 United States, Colorado Pfizer Investigational Site Aurora, Colorado, United States, 80045 United States, Georgia Pfizer Investigational Site Atlanta, Georgia, United States, 30308 Pfizer Investigational Site Atlanta, Georgia, United States, 30322 United States, Maryland Pfizer Investigational Site Bethesda, Maryland, United States, 20892 United States, Massachusetts Pfizer Investigational Site Boston, Massachusetts, United States, 02114 Pfizer Investigational Site Boston, Massachusetts, United States, 02115 Pfizer Investigational Site Boston, Massachusetts, United States, 02215 United States, Michigan Pfizer Investigational Site Detroit, Michigan, United States, 48201 Pfizer Investigational Site Farmington Hills, Michigan, United States, 48334 Collapse <<
NCT00553254	Carcinoma, Non Small Cell Lung	Phase 1 Phase 2	Completed	-	Korea, Republic of ... more >> Pfizer Investigational Site Seoul, Korea, Republic of, 110-744 Pfizer Investigational Site Seoul, Korea, Republic of, 120-752 Pfizer Investigational Site Seoul, Korea, Republic of, 135-710 Collapse <<
NCT00225121	Neoplasms	Phase 1	Completed	-	United States, California ... more >> Pfizer Investigational Site Los Angeles, California, United States, 90095 Pfizer Investigational Site Santa Monica, California, United States, 90404 United States, Colorado Pfizer Investigational Site Aurora, Colorado, United States, 80045 United States, Massachusetts Pfizer Investigational Site Boston, Massachusetts, United States, 02114 Pfizer Investigational Site Boston, Massachusetts, United States, 02115 Netherlands Pfizer Investigational Site Amsterdam, Netherlands, 1066 CX Collapse <<
NCT00971191	Non-Small Cell Lung Cancer (NS... more >>CLC) Collapse <<	Phase 1	Terminated(See termination rea... more >>son in detailed description.) Collapse <<	-	United States, Alabama ... more >> Pfizer Investigational Site Birmingham, Alabama, United States, 35294 United States, California Pfizer Investigational Site Los Angeles, California, United States, 90048 Pfizer Investigational Site Los Angeles, California, United States, 90095 Collapse <<
NCT00728390	Carcinoma, Non-Small Cell ... more >> Neoplasm Metastasis Collapse <<	Phase 1	Completed	-	United States, New York ... more >> Pfizer Investigational Site Amherst, New York, United States, 14221 Pfizer Investigational Site Buffalo, New York, United States, 14263 United States, Texas Pfizer Investigational Site San Antonio, Texas, United States, 78229 France Pfizer Investigational Site Villejuif, France, 94805 Spain Pfizer Investigational Site Madrid, Spain, 28050 Collapse <<
NCT01116843	Oral Cavity Cancer	Phase 1 Phase 2	Completed	-	Canada, Ontario ... more >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Collapse <<
NCT01441128	Carcinoma, Non-Small Cell Lung... more >> Adenocarcinoma Carcinoma, Squamous Cell Carcinoma, Large Cell Collapse <<	Phase 1	Terminated	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<
NCT01121575	-	-	Completed	-	-
NCT00728468	Advanced Malignant Solid Tumor... more >>s Collapse <<	Phase 1	Completed	-	United States, New York ... more >> Roswell Park Cancer Institute Buffalo, New York, United States, 14263 United States, Texas South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 Collapse <<
NCT00999817	Healthy Volunteers	Phase 1	Completed	-	Belgium ... more >> Pfizer Investigational Site Bruxelles, Belgium, 1070 Collapse <<
NCT00728468	-	-	Completed	-	-
NCT01034748	Carcinoma, Non-Small-Cell Lung	Phase 1	Completed	-	United States, Washington ... more >> Pfizer Investigational Site Tacoma, Washington, United States, 98418 Collapse <<
NCT01449201	Head Neck Cancer Squamous Cell... more >> Metastatic Head Neck Cancer Squamous Cell Recurrent Collapse <<	Phase 2	Completed	-	Korea, Republic of ... more >> Chilgok Kyungpook National University Hospital Daegu, Korea, Republic of Dongsan Medical Center Daegu, Korea, Republic of Severance Hospital Seoul, Korea, Republic of, 120-752 Asan Medical Center Seoul, Korea, Republic of Samsung Medical Center Seoul, Korea, Republic of Seoul National University Hospital Cancer Center Seoul, Korea, Republic of Collapse <<
NCT01112527	Glioblastoma ... more >>GBM Glioblastoma Multiforme Collapse <<	Phase 2	Completed	-	United States, Massachusetts ... more >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Michigan Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, Ohio Cleveland Clinic Cleveland, Ohio, United States, 44195 Collapse <<
NCT01465802	-	-	Completed	-	-
NCT00818441	Carcinoma, Non-small Cell	Phase 2	Completed	-	-
NCT02039336	Colorectal Cancer	Phase 1 Phase 2	Recruiting	December 2019	Netherlands ... more >> The Netherlands Cancer Institute Recruiting Amsterdam, Netherlands, 1066CX Contact: F opdam, MD, PhD +31 20 512 2446 f.opdam@nki.nl Erasmus Medical Center Cancer Institute Recruiting Rotterdam, Netherlands, 3015CE University Medical Center Utrecht Recruiting Utrecht, Netherlands, 3584CX Collapse <<
NCT01465802	Non Small Cell Lung Cancer (NS... more >>CLC) Collapse <<	Phase 2	Completed	-	-
NCT01702506	Healthy Volunteers	Phase 1	Completed	-	Belgium ... more >> Pfizer Investigational Site Bruxelles, Belgium, B-1070 Collapse <<
NCT01360554	Non-Small Cell Lung Cancer	Phase 3	Completed	-	-
NCT01484847	Head and Neck Squamous Cell Ca... more >>rcinoma Collapse <<	Not Applicable	Completed	-	Canada, Ontario ... more >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Collapse <<
NCT01520870	Glioblastoma ... more >>Brain Tumor, Recurrent Collapse <<	Phase 2	Completed	-	Spain ... more >> Hospital Universitari Germans Trias I Pujol de Badalona Badalona, Barcelona, Spain, 08916 Institut Català D'Oncologia L'Hospitalet (Ico) L'Hospitalet de Llobregat, Barcelona, Spain, 08908 Hospital Universitario A Coruña A Coruna, Coruña (A), Spain, 15006 Hospital Del Mar Barcelona, Spain, 08003 Hospital de La Santa Creu I Sant Pau Barcelona, Spain, 08025 Complejo Hospitalario Regional Virgen de Las Nieves Granada, Spain, 18004 Hospital Ramón Y Cajal Madrid, Spain, 28034 Hospital Clínico San Carlos Madrid, Spain, 28040 Hospital Universitario 12 de Octubre Madrid, Spain, 28041 Hospital Regional Universitario de Malaga Malaga, Spain Complejo Hospitalario Universitario Insular-Materno Infantil Palmas de Gran Canaria, Spain, 35016 Hospital Universitario Y Politécnico La Fe Valencia, Spain, 46009 Collapse <<
NCT01152853	Advanced Gastric Cancer ... more >> HER2 Collapse <<	Phase 2	Completed	-	Korea, Republic of ... more >> Seoul National University Hospital Seoul, Korea, Republic of, 110-744 Collapse <<
NCT01858389	-	-	Completed	-	-
NCT02382796	NSCLC	Phase 2	Active, not recruiting	May 2019	Japan ... more >> Kanazawa University Hospital Kanazawa City, Ishikawa, Japan, 9208641 Kurashiki Central Hospital Kurashiki, Okayama, Japan, 710-8602 Osaka City General Hospital Department of Clinical Oncology Osaka-city, Osaka, Japan, 534-0021 Kindai University Hospital Osakasayama, Osaka, Japan, 589-8511 Shizuoka Cancer Center Suntougun, Shizuoka, Japan, 411-8777 Cancer Institute Hospital,Japanese Foundation for Cancer Research Koto-Ku, Japan, 135-8550 Collapse <<
NCT01571388	Healthy Other... more >>wise Healthy Volunteers With Mild or Moderate Hepatic Dysfunction Collapse <<	Phase 1	Completed	-	United States, California ... more >> Pfizer Investigational Site Anaheim, California, United States, 92801 United States, Florida Pfizer Investigational Site South Miami, Florida, United States, 33143 Collapse <<
NCT00818441	-	-	Completed	-	-
NCT01360554	-	-	Completed	-	-
NCT02047747	Brain Cancer	Phase 2	Terminated(slow enrollment)	-	United States, California ... more >> UCSD Moores Cancer Center La Jolla, California, United States, 92093-0698 Collapse <<
NCT01774721	-	-	Active, not recruiting	-	-
NCT01774721	Non-small Cell Lung Cancer Wit... more >>h EGFR-Activating Mutations Collapse <<	Phase 3	Active, not recruiting	March 29, 2019	-
NCT03755102	EGFR Gene Mutation ... more >> Lung Cancer Lung Cancer Metastatic Collapse <<	Early Phase 1	Recruiting	November 2019	United States, New Jersey ... more >> Memoral Sloan Kettering Basking Ridge Recruiting Basking Ridge, New Jersey, United States, 07920 Contact: Helen Yu, MD 646-888-4274 Memoral Sloan Kettering Monmouth Recruiting Middletown, New Jersey, United States, 07748 Contact: Helen Yu, MD 646-888-4274 United States, New York Memorial Sloan Kettering Cancer Center @ Commack Recruiting Commack, New York, United States, 11725 Contact: Helen Yu, MD 646-888-4274 Memoral Sloan Kettering Westchester Recruiting Harrison, New York, United States, 10604 Contact: Helen Yu, MD 646-888-4274 Memorial Sloan - Kettering Cancer Center Recruiting New York, New York, United States, 10021 Contact: Helen Yu, MD 646-888-4274 Memorial Sloan Kettering @ Rockville Recruiting Rockville Centre, New York, United States, 11570 Contact: Helen Tu, MD 646-888-4274 Collapse <<
NCT02047747	-	-	Terminated(slow enrollment)	-	-
NCT01737008	Squamous Cell Carcinoma of the... more >> Head and Neck Collapse <<	Phase 1	Completed	-	Canada, Ontario ... more >> Princess Margaret Cancer Centre Toronto, Ontario, Canada, M5G 2M9 Collapse <<
NCT01796327	Healthy Volunteers	Phase 1	Completed	-	United Kingdom ... more >> Pfizer Investigational Site Ruddington Fields, Nottingham, United Kingdom, NG11 6JS Collapse <<
NCT02097433	Healthy	Phase 1	Completed	-	China ... more >> Peking Union Medical College Hospital Beijing, China, 100032 Collapse <<
NCT01728233	Penile Neoplasms ... more >> Carcinoma, Squamous Cell Collapse <<	Phase 2	Recruiting	February 15, 2018	Italy ... more >> Fondazione IRCCS Istituto Nazionale dei Tumori Recruiting Milan, Italy, 20133 Collapse <<
NCT02268747	Skin Squamous Cell Cancer	Phase 2	Unknown	November 2016	Italy ... more >> Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Milan, Italy, 20133 Collapse <<
NCT01858389	Non-small Cell Lung Cancer	Phase 2	Completed	-	United States, California ... more >> Tower Hematology Oncology Medical Group Beverly Hills, California, United States, 90211 Cedars-Sinai Medical Center, Samuel Oschin Comprehensive Cancer Institute Los Angeles, California, United States, 90048 United States, District of Columbia Georgetown University Hospital-Lombardi Comprehensive Cancer Center Washington, D.C., District of Columbia, United States, 20007 Georgetown University Medical Center Department of Pharmacy, Research Washington, D.C., District of Columbia, United States, 20007 United States, New York Memorial Sloan-Kettering Cancer Center-Rockefeller Outpatient Pavilion New York, New York, United States, 10022 United States, Pennsylvania Investigational Drug Service, Hillman Cancer Center Pittsburgh, Pennsylvania, United States, 15232 University of Pittsburgh Medical Center Pittsburgh, Pennsylvania, United States, 15232 UPMC Hillman Cancer Center Pittsburgh, Pennsylvania, United States, 15232 United States, Texas UT Southwestern Medical Center-Simmons Cancer Center Pharmacy Dallas, Texas, United States, 75390-9015 UT Southwestern Medical Center Dallas, Texas, United States, 75390 UT Southwestern University Hospital - William P. Clements, Jr. Dallas, Texas, United States, 75390 UT Southwestern University Hospital - Zale Lipshy Dallas, Texas, United States, 75390 Korea, Republic of Severance Hospital, Yonsei University Health System Seoul, Korea, Republic of, 120-752 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Collapse <<
NCT01918761	Non Small Cell Lung Cancer	Phase 1	Suspended(poor accrual)	September 15, 2018	Austria ... more >> Medizinische Universität Graz Klinische Abteilung für Onkologie Graz, Austria Universitätsklinik für Innere Medizin I Innsbruck, Austria Collapse <<

靶点	Description	IC50
EGFR		IC50:6nM
ERBB4		IC50:73.7nM
HER2		IC50:45.7nM

达克替尼 Catalog No. CSN13899

靶点选择性

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