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

194423-15-9

194423-15-9 structure

Name: PD168393
Chemical Name: N-[4-(3-bromoanilino)quinazolin-6-yl]prop-2-enamide
CAS Number: 194423-15-9
Molecular Formula: C₁₇H₁₃BrN₄O
Molecular Weight: 369.215
Catalog: Biochemical Inhibitor Protein tyrosine kinase
Create Date: 2018-12-25 20:55:18
Modify Date: 2024-01-02 16:49:54
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
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

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

79-10-7

169205-78-1

~43%

194423-15-9

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

256409-20-8

~84%

194423-15-9

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

256409-24-2

~56%

194423-15-9

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

256409-22-0

~49%

194423-15-9

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

814-68-6

169205-78-1

~11%

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

169205-78-1

194423-15-9

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

17420-30-3

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

169205-77-0

194423-15-9

Precursor 5
79-10-7 169205-78-1 814-68-6 17420-30-3
169205-77-0
DownStream 0

56-41-7	108-65-6
56-35-9	64-17-5
67-56-1	108-88-3
141-78-6	1310-73-2
13463-67-7	1333-86-4