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Key Documents

PZ0330

Sigma-Aldrich

Dacomitinib

≥98% (HPLC)

Synonym(s):

(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide, PF-00299804, PF-00299804-03, PF-299

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About This Item

Empirical Formula (Hill Notation):
C24H25ClFN5O2
CAS Number:
1110813-31-4
Molecular Weight:
469.94
UNSPSC Code:
41106609
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

room temp

InChI

1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+

InChI key

LVXJQMNHJWSHET-AATRIKPKSA-N

Biochem/physiol Actions

Dacomitinib (PF-00299804) is an irreversible EGFR inhibitor and antineoplastic. It is a potent inhibitor of HER-1 (EGFR), -2 and -4 tyrosine kinase with IC50s of 6.0, 45.7 and 73.7 nM respectively for EGFR, ERBB2 and ERBB4. Dacomitinib is believed to irreversibly inhibit erbB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of erbB family members.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Yutaro Yamamoto et al.
Acta histochemica et cytochemica, 52(6), 101-106 (2020-02-01)
Dacomitinib, a second-generation tyrosine kinase inhibitor, was irreversible inhibitor forming covalent bonds with the kinase domains of EGFR and other ErbB family receptors. Dacomitinib has been approved for the treatment of locally advanced or metastatic non-small cell lung cancer. In
Jeffrey A Engelman et al.
Cancer research, 67(24), 11924-11932 (2007-12-20)
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors gefitinib and erlotinib are effective treatments for a subset of non-small cell lung cancers. In particular, cancers with specific EGFR-activating mutations seem to be the most sensitive to these agents. However, despite
Personalizing therapy in an epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer using PF-00299804 and trastuzumab.
Ronan J Kelly et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 28(28), e507-e510 (2010-08-04)
Andrea J Gonzales et al.
Molecular cancer therapeutics, 7(7), 1880-1889 (2008-07-09)
Signaling through the erbB receptor family of tyrosine kinases contributes to the proliferation, differentiation, migration, and survival of a variety of cell types. Abnormalities in members of this receptor family have been shown to play a role in oncogenesis, thus
Abram Calderon et al.
Oncotarget, 11(46), 4224-4242 (2020-11-28)
KSHV-associated cancers have poor prognoses and lack therapeutics that selectively target viral gene functions. We developed a screening campaign to identify known drugs that could be repurposed for the treatment of KSHV-associated cancers. We focused on primary effusion lymphoma (PEL)

Articles

Irreversible Inhibitors

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