Catalog Number: 4193
Chemical Name: 4-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-N-2[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxy-2-quinazolinamine hydrochloride
Biological Activity
High affinity P-glycoprotein (P-gp) inhibitor (Ki values are 58 and 94 nM for mouse Pgp1a and Pgp1b isoforms). Inhibits calcein-AM uptake in MDR1-transfected MDCKII cells (IC50 = 0.5 μM) and prazosin transport in BCRP-transfected MDCKII cells (IC50 = 1.5 μM). Displays weak or no inhibitory activity against MRP1, OATP1B1 and several major human P450 enzymes (IC50 > 50 μM).
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar.
    Taylor et al.
    Br.J.Cancer, 1999;81:783
  2. P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies.
    Wandel et al.
    Cancer Res., 1999;59:3944
  3. 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
    Kalgutkar et al.
    J.Pharm.Sci., 2009;98:4914

The citations listed below are publications that use Tocris products. Selected citations for CP 100356 hydrochloride include:

Showing Results 1 - 1 of 1

  1. Calcium and P-glycoprotein independent synergism between schweinfurthins and verapamil.
    Authors: Sheehy Et al.
    Acta Neuropathol Commun
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