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CB-1158 dihydrochloride
- Numidargistat dihydrochloride - INCB-01158 dihydrochloride
Axon 3738
- Parent CAS: 2095732-06-0
- Optical Purity: 99% e.e.
- Soluble in water
- MF: C11H22BN3O5.2HCl
- MW: 360.04
Description
CB-1158 dihydrochloride, also known as Numidargistat dihydrochloride, is a potent and orally active arginase inhibitor (with IC50 values of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2). It's an immuno-oncology agent that has shown potential in various cancer models, particularly by enhancing the immune response within the tumor microenvironment.
More Information
| Parent CAS No. | 2095732-06-0 |
|---|---|
| Chemical Name | (3R,4S)-3-amino-1-((S)-2-aminopropanoyl)-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid dihydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | [C@]1(N)(C(=O)O)CN(C([C@@H](N)C)=O)C[C@@H]1CCCB(O)O.Cl.Cl |&1:0,8,13,r| |
| MFCD | N.A. |
| 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 |
| InChiKey | ZZJLMZYUGLJBSO-LAEOZQHASA-N |
| CID | 131801114 |
| Short Description | Arginase inhibitor |
References
- M Works et al, Immuno-oncology agent CB-1158 is a potent and selective arginase inhibitor and causes an immune-mediated anti-tumor response. AACR; Cancer Res 2016; 76(14 Suppl); Abstract No 552.
- KP Papadopoulos et al. A first-in-Human Phase 1 Study of CB-1158, a Small Molecule Inhibitor of Arginase, as Monotherapy and in Combination with an Anti-PD-1 Checkpoint Inhibitor in Patients (pts) with Solid Tumors, J Clin Oncol 35, 2017 (suppl; abstr 3005).
- SM Steggerda 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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