| Identification | Back Directory | [Name]
5H-Pyrrolo[3,2-d]pyrimidine-4-carboxamide, 2-(1H-imidazol-1-yl)-N-[trans-4-(2-methoxyethoxy)cyclohexyl]- | [CAS]
2597933-17-8 | [Synonyms]
5H-Pyrrolo[3,2-d]pyrimidine-4-carboxamide, 2-(1H-imidazol-1-yl)-N-[trans-4-(2-methoxyethoxy)cyclohexyl]- | [Molecular Formula]
C19H24N6O3 | [MOL File]
2597933-17-8.mol | [Molecular Weight]
384.43 |
| Chemical Properties | Back Directory | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (650.31 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.41±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
RBN013209 is an orally active small molecule inhibitor of CD38 with an IC50 of 0.01 to 0.1 μM for human CD38. RBN013209 prevents the conversion of extracellular NAD+ to ADPR or cADPR in tumor cells and PBMCs. RBN013209 can be used in the study of tumor. In addition, RBN013209 enables CAR-T cells to maintain the naive state and central memory state, and decreases the expression of cell activation markers and exhaustion-related inhibitory receptors[1][2][3]. | [Biological Activity]
RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer. | [in vivo]
RBN013209 (Oral administration) has antitumor activity in mice[3]. | Animal Model: | Mice[3] | | Dosage: | / | | Administration: | Oral administration | | Result: | Resulted in dose-dependent elevation of NAD+ and reduction of ADPR in various tissues such as spleen and liver in na?ve mice.
Had antitumor activity that was associated with changes in NAD+ and ADPR in MC38 tumor model.
Had antitumor activity in combinationwith anti-PD-L1 therapy in B16-F10 tumor-bearing mice.
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| [References]
[1]. Laurie B. Schenkel, et al. Heterobicyclic amides as inhibitors of cd38. WO2021021986 A1. |
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