211555-04-3

211555-04-3 structure

Name: WHI-P154
Chemical Name: 2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
CAS Number: 211555-04-3
Molecular Formula: C₁₆H₁₄BrN₃O₃
Molecular Weight: 376.205
Catalog: Biochemical Inhibitor Tyrosine protein kinase/signal transducer and transcriptional activator inhibitor (JAK/STAT) JAK inhibitor
Create Date: 2018-10-09 11:39:33
Modify Date: 2024-01-05 18:54:56
WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.

Name	2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
Synonyms	2-Bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol Phenol, 2-bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]- WHI-P154 jak3 inhibitor ii 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol

Description	WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
Related Catalog	Research Areas >> Cancer
Target	EGFR:4 nM (IC50) JAK3:1.8 μM (IC50)
In Vitro	WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively[1]. WHI-P154 significantly enhances the sensitivity of ABCG2-overexpressing cells to its substrates. WHI-P154 (4 μM) moderately sensitizes ABCB1-overexpressing KB-C2 cells to its substrates whereas shows no sensitizing effect on ABCC1-, ABCC2 or ABCC10-mediated drug resistance. Moreover, WHI-P154 (4 μM) causes a significant increase in the intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells. WHI-P154 alters the expression levels rather than the localization of the ABCG2 protein in ABCG2-overexpressing cells[2].
References	[1]. Changelian PS, et al. The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7. Epub 2007 Dec 19. [2]. Zhang H, et al. WHI-P154 enhances the chemotherapeutic effect of anticancer agents in ABCG2-overexpressing cells. Cancer Sci. 2014 Aug;105(8):1071-8.

Density	1.6±0.1 g/cm3
Boiling Point	470.3±45.0 °C at 760 mmHg
Melting Point	230 °C
Molecular Formula	C₁₆H₁₄BrN₃O₃
Molecular Weight	376.205
Flash Point	238.2±28.7 °C
Exact Mass	375.021851
PSA	76.50000
LogP	4.15
Appearance	white to brown
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.703
Storage condition	Store at RT
Water Solubility	DMSO: soluble1mg/mL, clear (warmed)