2360851-29-0
2360851-29-0 structure
- Name: RBN012759
- Chemical Name: RBN012759
- CAS Number: 2360851-29-0
- Molecular Formula: C19H23FN2O3S
- Molecular Weight: 378.46
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2020-10-31 09:54:28
- Modify Date: 2024-01-09 23:10:28
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RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants[1].
| Name | RBN012759 |
|---|
| Description | RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants[1]. |
|---|---|
| Related Catalog | |
| Target |
PARP14:<3 nM (IC50) PARP4:10 μM (IC50) PARP5a:8 μM (IC50) PARP5b:10 μM (IC50) PARP6:4 μM (IC50) PARP7:4 μM (IC50) PARP8:20 μM (IC50) PARP10:1 μM (IC50) PARP11:1 μM (IC50) PARP12:5 μM (IC50) PARP15:3 μM (IC50) PARP16:6 μM (IC50) |
| In Vitro | RBN012759 (0.01-10 μM) decreases the MAR/PAR signal corresponding to PARP14 self MARylation and stabilizes PARP14 protein in a dose-dependent manner in human primary macrophages[1]. RBN012759 (0.1-10 μM) reduces IL-4 stimulated cytokine secretion in human primary macrophages[1]. |
| In Vivo | RBN012759 (500 mg/kg BID; p.o.) is well-tolerated in mice with repeat dosing[1]. RBN012759 (100 mg/kg; p.o.) exhibits moderate orally bioavailability (30%) and short plasma half-life (0.4 h) due to moderate clearance (54 mL/min/kg) and low steady-state volume of distribution (1.4 L/kg) in mice[1]. |
| References |
| Molecular Formula | C19H23FN2O3S |
|---|---|
| Molecular Weight | 378.46 |
| Storage condition | -20°C |