CB-1158 dihydrochloride (2095732-06-0 free base) Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

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.
Target activity	Arginases II:296 nM , Arginases I:86 nM
Synonyms	INCB01158 dihydrochloride, CB-1158 dihydrochloride
molecular weight	360.04
Molecular formula	C11H24BCl2N3O5
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	H2O: 50 mg/mL (138.87 mM)
References	1. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.

PeptideDB