PD168393

Modify Date: 2024-01-02 16:49:54

PD168393 structure	Common Name	PD168393
	CAS Number	194423-15-9	Molecular Weight	369.215
	Density	1.6±0.1 g/cm3	Boiling Point	571.1±50.0 °C at 760 mmHg
	Molecular Formula	C₁₇H₁₃BrN₄O	Melting Point	279℃
	MSDS	USA	Flash Point	299.2±30.1 °C

Use of PD168393

PD168393 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]

Name	N-[4-(3-bromoanilino)quinazolin-6-yl]prop-2-enamide
Synonym	More Synonyms

Description	PD168393 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 Catalog	Signaling Pathways >> Autophagy >> Autophagy Research 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.

Density	1.6±0.1 g/cm3
Boiling Point	571.1±50.0 °C at 760 mmHg
Melting Point	279℃
Molecular Formula	C₁₇H₁₃BrN₄O
Molecular Weight	369.215
Flash Point	299.2±30.1 °C
Exact Mass	368.027252
PSA	70.40000
LogP	3.72
Vapour Pressure	0.0±1.6 mmHg at 25°C
Index of Refraction	1.744
Storage condition	-20°C

RIDADR	NONH for all modes of transport

Acrylic acid

CAS#:79-10-7

N4-(3-Bromophen...

CAS#:169205-78-1

~43%

PD168393

CAS#:194423-15-9

Literature: Warner-Lambert Company Patent: US6344459 B1, 2002 ; Location in patent: Page column 48 ; US 6344459 B1

N/A

CAS#:256409-20-8

~84%

PD168393

CAS#:194423-15-9

Literature: Wyeth Patent: EP1100788 B1, 2005 ; Location in patent: Page/Page column 7 ;

4-(3-bromopheny...

CAS#:256409-24-2

~56%

PD168393

CAS#:194423-15-9

Literature: Wyeth Patent: EP1100788 B1, 2005 ; Location in patent: Page/Page column 9-10 ;

4-(3-bromo phen...

CAS#:256409-22-0

~49%

PD168393

CAS#:194423-15-9

Literature: Wyeth Patent: EP1100788 B1, 2005 ; Location in patent: Page/Page column 8 ;

Acrylyl chloride

CAS#:814-68-6

N4-(3-Bromophen...

CAS#:169205-78-1

~11%

PD168393

CAS#:194423-15-9

Literature: Pawar, Vijaykumar G.; Sos, Martin L.; Rode, Haridas B.; Rabiller, Matthias; Heynck, Stefanie; Van Otterlo, Willem A. L.; Thomas, Roman K.; Rauh, Daniel Journal of Medicinal Chemistry, 2010 , vol. 53, # 7 p. 2892 - 2901

N4-(3-Bromophen...

CAS#:169205-78-1

PD168393

CAS#:194423-15-9

Literature: American Cyanamid Company Patent: EP787722 A1, 1997 ; Title/Abstract Full Text Show Details Wyeth Holdings Corporation Patent: EP980244 B1, 2003 ;

2-Cyano-4-nitro...

CAS#:17420-30-3

PD168393

CAS#:194423-15-9

Literature: Tsou; Mamuya; Johnson; Reich; Gruber; Ye; Nilakantan; Shen; Discafani; DeBlanc; Davis; Koehn; Greenberger; Wang; Wissner Journal of Medicinal Chemistry, 2001 , vol. 44, # 17 p. 2719 - 2734

N-(3-bromopheny...

CAS#:169205-77-0

PD168393

CAS#:194423-15-9

Precursor 5
CAS#:79-10-7 Acrylic acid CAS#:169205-78-1 N4-(3-Bromophen... CAS#:814-68-6 Acrylyl chloride CAS#:17420-30-3 2-Cyano-4-nitro...
CAS#:169205-77-0 N-(3-bromopheny...
DownStream 0

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

DC Chemicals Limited
China
Product Name: PD168393
Price: $350.0/100mg $700.0/250mg $1500.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Price: $68/10mM*1mLinDMSO

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PD168393

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