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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | Inquiry | 6-8 weeks | |
50 mg | Inquiry | 6-8 weeks | |
100 mg | Inquiry | 6-8 weeks |
Description | CB-1158 is a potent and orally bioavailable inhibitor of arginase (IC50s: 86 and 296 nM for recombinant human arginase 1 and 2). |
In vitro | CB-1158 is not directly cytotoxic to murine cancer cell lines [1]. 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 shows no effect on NOS and it also shows potent inhibitory activity against arginase in human HepG2, K562 cell lines, and primary human hepatocytes (IC50s: 32, 139, 210 μM). |
In vivo | CB-1158 in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells. CB-1158 (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. |
Alias | INCB01158, CB-1158 |
Molecular Weight | 287.12 |
Formula | C11H22BN3O5 |
Cas No. | 2095732-06-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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