CP 100356 hydrochloride

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Cat.No. 4193 - CP 100356 hydrochloride | C31H36N4O6.HCl | CAS No. 142715-48-8
Description: P-gp inhibitor
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
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

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).

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 597.1
Formula C31H36N4O6.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 142715-48-8
PubChem ID 71312025
InChI Key WWCHXVYTCMPAMV-UHFFFAOYSA-N
Smiles COC2=CC1=C(N3CCC(C=C(OC)C(OC)=C5)=C5C3)N=C(NCCC4=CC=C(OC)C(OC)=C4)N=C1C=C2OC.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.94 20

Preparing Stock Solutions

The following data is based on the product molecular weight 597.1. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.67 mL 8.37 mL 16.75 mL
5 mM 0.33 mL 1.67 mL 3.35 mL
10 mM 0.17 mL 0.84 mL 1.67 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

Molarity Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: pfizer CP100356 p-gp p-glycoprotein abcb1 atp binding cassette multidrug transporters inhibitors inhibits Multidrug Transporters

1 Citation for CP 100356 hydrochloride

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 verapamil. Acta Neuropathol Commun 16 1259 PMID: 26046259


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