CP 100356 hydrochloride

Name: CP 100356 hydrochloride
Brand: Tocris Bioscience
SKU: 4193

Tocris Bioscience, part of Bio-Techne | Catalog # 4193

Citations (1)

COA / SDS

P-gp inhibitor

Key Product Details

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)
Molecular Weight:	597.1

View Full Technical Details for CP 100356 hydrochloride

Technical Data
Citations

Biological Activity for CP 100356 hydrochloride

CP 100356 hydrochloride is a high affinity P-glycoprotein (P-gp) inhibitor (K_i 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 for CP 100356 hydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for CP 100356 hydrochloride

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

Preparing Stock Solutions for CP 100356 hydrochloride

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

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References for CP 100356 hydrochloride

References are publications that support the biological activity of the product.

Wandel P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 1999 PMID: 10463589
Kalgutkar 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. 2009 PMID: 19373887
Taylor The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br.J.Cancer 1999 PMID: 10555746