RBN-2397 New

Product Description

RBN-2397 is a potent and selective PARP7 inhibitor (IC₅₀< 3 nM, K_D = 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.

Solubility

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.

Select a batch to recalculate based on the batch molecular weight:

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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

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