Rucaparib Phosphate

Rucaparib Phosphate is a potent PARP inhibitor API that has been developed as a targeted therapy for BRCA-mutant cancers. As a tricyclic indole PARP1 inhibitor, Rucaparib Phosphate selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, promoting genomic instability and apoptosis in cancer cells. The phosphate salt form of Rucaparib Phosphate provides enhanced aqueous solubility and improved physicochemical properties compared to the free base, facilitating pharmaceutical formulation and oral bioavailability. In pharmaceutical manufacturing, Rucaparib Phosphate requires stringent quality control to ensure batch-to-batch consistency and therapeutic efficacy. As a PARP inhibitor, Rucaparib Phosphate exploits synthetic lethality in tumors with BRCA1/2 mutations, representing a clinically validated approach in precision oncology. For generic manufacturers and research institutions, Rucaparib Phosphate represents both a high-value therapeutic API and a compound of significant interest for PARP inhibitor drug discovery.

 

Product Parameters

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Parameter	Specification
Product Name	Rucaparib Phosphate
CAS Number	459868-92-9
Molecular Formula	C₁₉H₂₁FN₃O₅P
Molecular Weight	421.37 g/mol
Appearance	Yellow solid
Melting Point	＞173 °C
Storage Condition	Sealed in dry,Room Temperature

 

Bioactivity

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Rucaparib (AG-014699, PF-01367338) is a PARP inhibitor with a Ki value of 1.4 nM for PARP1 in cell-free assays and binding affinity to the remaining eight PARP sites. Phase 3 clinical trial.

 

In Vitro Study

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AG-014699 effectively inhibits purified full-length human PARP-1 and demonstrates potent PARP-inhibitory effects in LoVo and SW620 cells. As the phosphate derivative of AG14447, it is the first PARP inhibitor to be combined with temozolomide for clinical trials. The radiosensitizing effect of AG-014699 stems from inhibition of downstream NF-κB activation and SSB repair. This compound targets DNA-damage-induced NF-κB activation while overcoming the toxicity associated with conventional NF-κB inhibitors without impairing other critical inflammatory responses. At a concentration of 1 μM, AG-014699 inhibited PARP-1 activity by 97.1% in D283 Med cells. In NB-1691, SH-SY-5Y, and SKNBE(2c) cells, AG-014699 significantly enhanced the cytotoxicity of topotecan and temozolomide.

 

In Vivo Studies

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AG-014699 is non-toxic and significantly enhances temozolomide-induced tumor growth inhibition (TGD) in DNA repair proteins of D384Med xenografts. Pharmacokinetic studies demonstrated the presence of AG-014699 in brain tissue, suggesting its potential for treating intracranial malignancies. In vivo model studies (NB1691 and SHSY5Y xenografts) revealed that AG-014699 enhances the anticancer efficacy of temozolomide, inducing complete and sustained tumor regression.

 

Contact Us

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When you need Rucaparib Phosphate with the quality, documentation, and supply reliability your PARP inhibitor program demands, Cosperpharm is here to help.