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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $215 | Backorder | |
10 mg | $372 | Backorder | |
25 mg | $724 | Backorder |
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 | Arginases II:296 nM , Arginases I: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. |
Alias | INCB01158 dihydrochloride, CB-1158 dihydrochloride |
Molecular Weight | 360.04 |
Formula | C11H24BCl2N3O5 |
Cas No. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 50 mg/mL (138.87 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O
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