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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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N646407-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $100.90 | |
N646407-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $250.90 | |
N646407-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $450.90 |
Synonyms | CB1158, 2HCl | NUMIDARGISTAT [INN] | NUMIDARGISTAT [WHO-DD] | numidargistatum | CB 1158 | CS-8064 | WHO 11086 | 2095732-06-0 | NSC803247 | NSC-803247 | Numidargistat | DB15286 | (3R,4S)-1-(L-alanyl)-3-amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid |
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Specifications & Purity | ≥98% |
Biochemical and Physiological Mechanisms | Numidargistat (CB-1158) is a potent and orally active inhibitor of arginase , with IC 50 s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2 , respectively. Immuno-oncology agent. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | Numidargistat (CB-1158) is a potent and orally active inhibitor of arginase , with IC 50 s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2 , respectively. Immuno-oncology agent In Vitro Numidargistat is a potent and orally-bioavailable inhibitor of arginase, with IC 50 s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC 50 s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC 50 , 122 nM). Numidargistat also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC 50 s of 32, 139, 210 μM, respectively. Numidargistat show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 86 nM (Arginase 1), 296 nM (Arginase 2) |
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IUPAC Name | (3R,4S)-3-amino-1-[(2S)-2-aminopropanoyl]-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid |
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INCHI | InChI=1S/C11H22BN3O5/c1-7(13)9(16)15-5-8(3-2-4-12(19)20)11(14,6-15)10(17)18/h7-8,19-20H,2-6,13-14H2,1H3,(H,17,18)/t7-,8-,11-/m0/s1 |
InChi Key | ZZJLMZYUGLJBSO-LAEOZQHASA-N |
Canonical SMILES | B(CCCC1CN(CC1(C(=O)O)N)C(=O)C(C)N)(O)O |
Isomeric SMILES | B(CCC[C@H]1CN(C[C@]1(C(=O)O)N)C(=O)[C@H](C)N)(O)O |
Alternate CAS | 2095732-06-0 |
PubChem CID | 131801114 |
MeSH Entry Terms | (3R,4S)-3-amino-1-((2S)-2-aminopropanoyl)-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid;CB-1158 |
Molecular Weight | 287.12 |
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