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

Catalog No. T10692   CAS T10692
Synonyms: INCB01158 dihydrochloride, CB-1158 dihydrochloride

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).

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CB-1158 dihydrochloride (2095732-06-0 free base) Chemical Structure
CB-1158 dihydrochloride (2095732-06-0 free base), CAS T10692
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
Targets&IC50 Arginase 2:296 nM , Arginase 1:86 nM
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.
Synonyms INCB01158 dihydrochloride, CB-1158 dihydrochloride
Molecular Weight 360.04
Formula C11H24BCl2N3O5
CAS No. T10692

Storage

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

Solubility Information

H2O: 50 mg/mL (138.87 mM)

TargetMolReferences and Literature

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.

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Keywords

CB-1158 dihydrochloride (2095732-06-0 free base) T10692 Others CB 1158 dihydrochloride (2095732 06 0 free base) CB 1158 INCB01158 Dihydrochloride CB-1158 CB1158 INCB-01158 2095732-06-0 free base INCB 01158 Dihydrochloride INCB 01158 INCB01158 dihydrochloride CB 1158 Dihydrochloride CB-1158 dihydrochloride CB1158 Dihydrochloride INCB-01158 Dihydrochloride CB-1158 Dihydrochloride 2095732-06-0 CB1158 dihydrochloride (2095732060 free base) INCB01158 inhibitor inhibit

 

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