CAS 194423-15-9|PD168393

Introduction:Basic information about CAS 194423-15-9|PD168393, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NamePD168393
CAS Number194423-15-9Molecular Weight369.215
Density1.6±0.1 g/cm3Boiling Point571.1±50.0 °C at 760 mmHg
Molecular FormulaC17H13BrN4OMelting Point279℃
MSDSUSAFlash Point299.2±30.1 °C

Names

NameN-[4-(3-bromoanilino)quinazolin-6-yl]prop-2-enamide
SynonymMore Synonyms

PD168393 BiologicalActivity

DescriptionPD168393 is an potent, cell-permeable, irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773, inactive against insulin, PDGFR, FGFR and PKC. target: EGFRIC 50: 0.7 nM [1](1) PD 168393 inhibite EGFr autophosphorylation in A431 human epidermoid carcinoma cells with >9-fold greater potency than PD 174265.[1](2) PD 168393 decrease the production of TNF-α and phosphrylation of ERK1/2 and p38 induced by LPS in cardiomyocytes.[2](3) PD168393 completely inhibits AKT and ERK phosphorylation at concentrations as low as 0.03 umol/L.[3](4) PD168393 could induce apoptosis and inhibit cell growth in ErbB2 positive lung and breast cancer cell lines.[3](5) PD168393 disrupted MEK1/p44/42 ERK signaling in HaCaT cells as determined by inhibition of phospho-p44/42 ERK. [4]
Related CatalogSignaling Pathways >>Autophagy >>AutophagyResearch Areas >>Cancer
Target

EGFR:0.7 nM (IC50)

References

[1]. Fry DW et al. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7.

[2]. Sun X et al. The activation of EGFR promotes myocardial tumor necrosis factor-α production and cardiac failure in endotoxemia. Oncotarget. 2015 Nov 3;6(34):35478-95.

[3]. Li G et al. Modulation of ErbB2 blockade in ErbB2-positive cancers: the role of ErbB2 Mutations and PHLDA1. PLoS One. 2014 Sep 19;9(9):e106349.

[4]. White KJ et al. Irritant activation of epithelial cells is mediated via protease-dependent EGFR activation. J Invest Dermatol. 2011 Feb;131(2):435-42.

Chemical & Physical Properties

Density1.6±0.1 g/cm3
Boiling Point571.1±50.0 °C at 760 mmHg
Melting Point279℃
Molecular FormulaC17H13BrN4O
Molecular Weight369.215
Flash Point299.2±30.1 °C
Exact Mass368.027252
PSA70.40000
LogP3.72
Vapour Pressure0.0±1.6 mmHg at 25°C
Index of Refraction1.744
InChIKeyHTUBKQUPEREOGA-UHFFFAOYSA-N
SMILESC=CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Storage condition-20°C

Safety Information

RIDADRNONH for all modes of transport

Synonyms

2-Propenamide (N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]
nchembio866-comp2
pd 168393
2-Propenamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-
N-{4-[(3-Bromophenyl)amino]-6-quinazolinyl}acrylamide
PD168393
CAS 1285702-20-6|ML-167
CAS 247068-82-2|[(1S)-3-Methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]carbamic acid 1,1-dim
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