RBN-2397 New
Tocris Bioscience, part of Bio-Techne | Catalog # 9003
Potent and selective PARP7 inhibitor; induces antitumor immunity
Key Product Details
Description
Potent and selective PARP7 inhibitor; induces antitumor immunity
Product Description
RBN-2397 is a potent and selective PARP7 inhibitor (IC50D = 0.22 nM in a probe displacement assay; IC50 = 1 nM in a NanoBRET assay). It displays >500-fold selectivity over PARP12 and >50-fold selectivity over all other PARPs.RBN-2397 inhibits MARylation of multiple intracellular proteins in PARP7-overexpressing SK-MES-1 cells (IC50 = 2 nM), showing a 300-fold window over the inhibition of PARylation in PARP1-activated HeLa cells. It restores the Type I interferon (IFN) response in tumor cells and induces antitumor immunity dependent on Type I IFN and CD8 cells. Significantly increases the proportion of cells in the G0/G1 phase of the cell cycle. In xenograft models, it slows tumor growth (TGI: 49-67%), with complete tumor regression in the NCI-H1373 xenograft. RBN-2397 is orally bioavailable.Product Specifications
Molecular Weight
523.44
Formula
C20H23F6N7O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
5-[[(1S)-1-Methyl-2-[3-oxo-3-[4-[5-(trifluoromethyl)-2-pyrimidinyl]-1-piperazinyl]propoxy]ethyl]amino]-4-(trifluoromethyl)-3(2H)-pyridazinone
CAS Number
2381037-82-5
PubChem ID
146047148
InChI Key
UQZCQKXJAXKZQH-LBPRGKRZSA-N
SMILES
FC(F)(C1=C(C=NNC1=O)N[C@@H](C)COCCC(N2CCN(C3=NC=C(C(F)(F)F)C=N3)CC2)=O)F
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.17 | 50 | |
| Ethanol | 2.62 | 5 |
Preparing Stock Solutions
for RBN-2397
The following data is based on the product molecular weight 523.44
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.82 mL | 19.10 mL | 38.21 mL |
| 2.5 mM | 0.76 mL | 3.82 mL | 7.64 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.82 mL |
| 25 mM | 0.08 mL | 0.38 mL | 0.76 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Chen PARP7 inhibitors and AHR agonists act synergistically across a wide range of cancer models. Mol.Cancer.Ther 2025 PMID: 39313957
- Yang Induction of PARP7 creates a vulnerability for growth inhibition by RBN2397 in prostate cancer cells. Cancer Res.Comm. 2023 PMID: 37077937
- Gozgit PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity. Cancer Cell 2021 PMID: 34375612
Product Specific Notices for RBN-2397
For research use only
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