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Biological Activity:
Potent inhibitor of P-glycoprotein (P-gp), with Ki to be 58 and 94 nM for 1a and 1b isomers of P-gp; an in vivo probe to selectively assess MDR1/BCRP-mediated drug efflux.
References:
C Wandel et al. P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 1999, 59, 3944. [online]
JC Taylor et al. The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br. J. Cancer 1999, 81(5), 783-789. [online]
AS Kalgutkar et al. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J. Pharm. Sci. 2009, 98, 4914. [online]
Chemical Name: N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine hydrochloride
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