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3-deazaneplanocin A HCl

Name: 3-deazaneplanocin A HCl
Brand: TargetMol
SKU: T6360
Price: 87 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6360Cas No. 120964-45-6

3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor.

3-deazaneplanocin A HCl

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Purity: 98.9%

Catalog No. T6360Cas No. 120964-45-6

3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$87	In Stock	In Stock
5 mg	$296	In Stock	In Stock
10 mg	$455	In Stock	In Stock
25 mg	$813	In Stock	In Stock
50 mg	$1,190	-	In Stock
100 mg	$1,630	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.9%

Appearance:Solid

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	3-deazaneplanocin A HCl is both an S-adenosyl-l-homocysteine hydrolase inhibitor and an enhancer of zeste homolog 2(EZH2) inhibitor.
In vitro	EZH2 expression was detected by quantitative PCR in 15 PDAC cells, including seven primary cell cultures, showing that expression values correlated with their originator tumors (Spearman R(2) = 0.89, P = 0.01). EZH2 expression in cancer cells was significantly higher than in normal ductal pancreatic cells and fibroblasts. The 3-deazaneplanocin A HCl(5 μmol/L, 72-hour exposure) modulated EZH2 and H3K27me3 protein expression and synergistically enhanced the antiproliferative activity of gemcitabine, with combination index values of 0.2 (PANC-1), 0.3 (MIA-PaCa-2), and 0.7 (LPC006). The drug combination reduced the percentages of cells in G(2)-M phase (e.g., from 27% to 19% in PANC-1, P < 0.05) and significantly increased apoptosis compared with gemcitabine alone. Moreover, 3-deazaneplanocin A HCl enhanced the mRNA and protein expression of the nucleoside transporters hENT1/hCNT1. 3-deazaneplanocin A HCl decreased cell migration, which was additionally reduced by 3-deazaneplanocin A HCl/gemcitabine combination (-20% in LPC006, after 8-hour exposure, P < 0.05) and associated with increased E-cadherin mRNA and protein expression. Furthermore, 3-deazaneplanocin A HCl and 3-deazaneplanocin A HCl/gemcitabine combination significantly reduced the volume of PDAC spheroids growing in CSC-selective medium and decreased the proportion of CD133+ cells[2].
In vivo	The survival of NOD/SCID mice with AML induced by HL-60 cells significantly increased when treated with 3-deazaneplanocin A HCl and PS compared to PS, 3-deazaneplanocin A HCl, or vehicle alone (P < .05). Cotreatment did not increase weight loss. Median survival: control, 36 days; PS, 42 days; 3-deazaneplanocin A HCl, 43 days; 3-deazaneplanocin A HCl plus PS, 52 days. Combined treatment improved survival of NOD/SCID mice with leukemia caused by AML HL-60 cells[3].

Chemical Properties

Molecular Weight	298.73
Formula	C₁₂H₁₅ClN₄O₃
Cas No.	120964-45-6
Smiles	Cl.Nc1nccc2n(cnc12)C1C=C(CO)C(O)C1O
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 50 mg/mL (167.38 mM), Sonication is recommended.

DMSO: 150 mg/mL (502.13 mM), Sonication is recommended.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3475 mL	16.7375 mL	33.4750 mL	167.3752 mL
5 mM	0.6695 mL	3.3475 mL	6.6950 mL	33.4750 mL
10 mM	0.3348 mL	1.6738 mL	3.3475 mL	16.7375 mL
20 mM	0.1674 mL	0.8369 mL	1.6738 mL	8.3688 mL
50 mM	0.0670 mL	0.3348 mL	0.6695 mL	3.3475 mL
100 mM	0.0335 mL	0.1674 mL	0.3348 mL	1.6738 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc