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Merck
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Documenti fondamentali

PZ0330

Sigma-Aldrich

Dacomitinib

≥98% (HPLC)

Sinonimo/i:

(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

Formula empirica (notazione di Hill):
C24H25ClFN5O2
Numero CAS:
1110813-31-4
Peso molecolare:
469.94
Codice UNSPSC:
41106609
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

room temp

Stringa SMILE

Fc1c(cc(cc1)Nc2ncnc3c2cc(c(c3)OC)NC(=O)\C=C\CN4CCCCC4)Cl

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+
LVXJQMNHJWSHET-AATRIKPKSA-N

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Lot/Batch Number

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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
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
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

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