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CB-1158 dihydrochloride (2095732-06-0 free base)

Catalog No. T10692

CB-1158 dihydrochloride is an effective and orally active inhibitor of arginase (IC50s: 86 nM and 296 nM for recombinant human arginase 1 and 2).

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.

Pack Size	Price	Availability
5 mg	$215	Backorder
10 mg	$372	Backorder
25 mg	$724	Backorder

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Product Introduction

Bioactivity

Description	CB-1158 dihydrochloride is an effective and orally active inhibitor of arginase (IC50s: 86 nM and 296 nM for recombinant human arginase 1 and 2).
In vitro	CB-1158 inhibits native arginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate (IC50s: 178 nM, 116 nM, and 158 nM), and blocks Arg1 in cancer patient plasma (IC50: 122 nM). CB-1158 also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines, and primary human hepatocytes (IC50s: 32, 139, 210 μM). CB-1158 shows no effect on NOS and not directly cytotoxic to murine cancer cell lines.
In vivo	CB-1158 (100 mg/kg, p.o., twice per day) decreases the number of myeloid cells and increases tumor-infiltrating cytotoxic cells in mice. CB-1158 in combination with LY 188011 inhibits tumor growth in mice bearing CT26 cancer cells.
Alias	INCB01158 dihydrochloride, CB-1158 dihydrochloride

Chemical Properties

Molecular Weight	360.04
Formula	C11H24BCl2N3O5
Cas No.

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (138.87 mM)

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	2.7775 mL	13.8873 mL	27.7747 mL	138.8735 mL
5 mM	0.5555 mL	2.7775 mL	5.5549 mL	27.7747 mL
10 mM	0.2777 mL	1.3887 mL	2.7775 mL	13.8873 mL
20 mM	0.1389 mL	0.6944 mL	1.3887 mL	6.9437 mL
50 mM	0.0555 mL	0.2777 mL	0.5555 mL	2.7775 mL
100 mM	0.0278 mL	0.1389 mL	0.2777 mL	1.3887 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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

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