2381037-82-5
2381037-82-5 structure
- Name: RBN-2397
- Chemical Name: RBN-2397
- CAS Number: 2381037-82-5
- Molecular Formula: C20H23F6N7O3
- Molecular Weight: 523.43
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2020-06-01 16:16:45
- Modify Date: 2024-01-12 10:50:44
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RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2].
| Name | RBN-2397 |
|---|
| Description | RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2]. |
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| Related Catalog | |
| Target |
PARP-7:3 nM (IC50) PARP-7:1 nM (Kd) |
| In Vitro | RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells[2]. RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells[2]. RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM[2]. Cell Proliferation Assay[2] Cell Line: NCI-H1373 lung cancer cells Concentration: 0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM Incubation Time: 24 hours Result: Blocked cell proliferation. Western Blot Analysis[2] Cell Line: NCI-H1373 lung cancer cells Concentration: 0.4 nM-1 μM Incubation Time: 24 hours Result: Increased p-STAT1 protein expression. |
| In Vivo | RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice[2]. RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg[2]. The half-life (t1/2) of RBN-2397 in vivo is 325 mins[2]. Animal Model: CB17 SCID mice with NCI-H1373 xenografts[2] Dosage: 3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration; once daily; 24-32 days Result: Decreased tumor volume and exerted anti-tumor effects. |
| References |
[1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency |
| Density | 1.53±0.1 g/cm3(Predicted) |
|---|---|
| Molecular Formula | C20H23F6N7O3 |
| Molecular Weight | 523.43 |
| Storage condition | -20°C |