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CP 100356 hydrochloride is a 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).
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 597.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||8.37 mL||41.87 mL||83.74 mL|
|1 mM||1.67 mL||8.37 mL||16.75 mL|
|2 mM||0.84 mL||4.19 mL||8.37 mL|
|10 mM||0.17 mL||0.84 mL||1.67 mL|
References are publications that support the biological activity of the product.
Taylor et al (1999) The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br.J.Cancer 81 783 PMID: 10555746
Wandel et al (1999) P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 59 3944 PMID: 10463589
Kalgutkar et al (2009) 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 J.Pharm.Sci. 98 4914 PMID: 19373887
If you know of a relevant reference for CP 100356 hydrochloride, please let us know.
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Citations are publications that use Tocris products. Selected citations for CP 100356 hydrochloride include:
Sheehy et al (2015) Calcium and P-glycoprotein independent synergism between schweinfurthins and vera. Acta Neuropathol Commun 16 1259 PMID: 26046259
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.