Antitumor agent-101

Name: Antitumor agent-101
Brand: TargetMol
SKU: T79249
Rating: 4.5 (1 reviews)

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Catalog No. T79249Cas No. 2848632-52-8

Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].

Antitumor agent-101

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Catalog No. T79249Cas No. 2848632-52-8

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	8-10 weeks	8-10 weeks
50 mg	$1,980	8-10 weeks	8-10 weeks
100 mg	$2,500	8-10 weeks	8-10 weeks

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

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Product Introduction

Bioactivity

Description	Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].
Targets&IC50	G9a:8.5 nM, GLP:5.5 nM
In vitro	Antitumor agent-101 (Compound 27) (0-5 μM; 48 hours) inhibits proliferation and colony formation in PANC-1 and MDA-MB-231 cells [1]. Furthermore, Antitumor agent-101 (0-10 μM; 0-96 hours) effectively reduces H3K9me2 levels in these cells in a concentration- and time-dependent manner.
In vivo	Antitumor agent-101 (Compound 27), administered at 2 mg/kg via intraperitoneal injection five times per week, inhibits the growth of PANC-1 xenograft tumors by suppressing the methyltransferase activity of G9a/GLP [1]. Additionally, this compound demonstrates a peak plasma concentration (Cmax) of 316 ng/mL and a mean residence time (MRT) of 0.61 hours [1].

Chemical Properties

Molecular Weight	482.62
Formula	C₂₆H₃₈N₆O₃
Cas No.	2848632-52-8
Smiles	N(C=1C2=C(C=C(OCCCN3CCCC3)C(OC)=C2)N=C(N(C(C=C)=O)C)N1)C4CCN(C)CC4

Storage & Solubility Information

Storage

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

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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