Pidnarulex (CX-5461) is a small-molecule inhibitor that selectively targets RNA polymerase I–mediated rRNA synthesis, exhibiting potent anticancer activity, particularly in tumors with defective homologous recombination (HR) repair mechanisms such as BRCA1/2 mutations. It stabilizes G-quadruplex DNA structures and induces replication stress and DNA damage, leading to synthetic lethality in HR-deficient cancer cells. Preclinical studies have shown nanomolar potency against a range of HR-deficient tumor cell lines, with GI₅₀ values typically in the range of 50–150 nM. In vivo, CX-5461 has demonstrated significant tumor regression in BRCA-deficient xenograft models
MedKoo Cat#: 413396
Name: Pidnarulex HCl
CAS#: 2101314-20-7 (HCl)
Chemical Formula: C27H28ClN7O2S
Exact Mass: 0.0000
Molecular Weight: 550.08
Elemental Analysis: C, 58.95; H, 5.13; Cl, 6.44; N, 17.82; O, 5.82; S, 5.83
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 550.08 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |