| Identification | Back Directory | [Name]
CB-1158 | [CAS]
2095732-06-0 | [Synonyms]
INCB01158
Numidargistat
Numidargistat (CB1158, INCB01158)
Numidargistat 2HCl (CB1158, INCB01158)
(3R,4S)-1-(L-alanyl)-3-amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid
3-Pyrrolidinecarboxylic acid, 3-amino-1-[(2S)-2-amino-1-oxopropyl]-4-(3-boronopropyl)-, (3R,4S)- | [Molecular Formula]
C11H22BN3O5 | [MOL File]
2095732-06-0.mol | [Molecular Weight]
287.12 |
| Chemical Properties | Back Directory | [Boiling point ]
574.1±60.0 °C(Predicted) | [density ]
1.299±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
2.13±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
(3R,4S)-3-Amino-1-[(2S)-2-amino-1-oxopropyl]-4-(3-boronopropyl)-3-pyrrolidinecarboxylic Acid Dihydrochloride is a salt analog of (3R,4S)-3-Amino-1-[(2S)-2-amino-1-oxopropyl]-4-(3-boronopropyl)-3-pyrrolidinecarboxylic Acid (CAS# 2095732-06-0), which inhibits arginase 1 (Arg1) enzyme and blocks myeloid cell-??mediated immune suppression in the tumor microenvironment. | [in vivo]
Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells[1]. |
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