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Merck
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Principaux documents

PZ0330

Sigma-Aldrich

Dacomitinib

≥98% (HPLC)

Synonyme(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

Formule empirique (notation de Hill):
C24H25ClFN5O2
Numéro CAS:
1110813-31-4
Poids moléculaire :
469.94
Code UNSPSC :
41106609
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

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+

Clé InChI

LVXJQMNHJWSHET-AATRIKPKSA-N

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

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
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)
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
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)

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