RP-1664

• Description :

  RP-1664 is a selective and orally active PLK4 inhibitor with an IC50 of 3 nM. RP-1664 demonstrates exquisite selectivity over related kinases, including AURKA/B and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells and leads an accumulation of PLK4 and p21 protein. RP-1664 demonstrates increased sensitivity in TRIM37-high-expressing cells or tumors. RP-1664 exhibits anti-tumor activity in breast cancer and neuroblastoma research[1][2].

• UNSPSC :

  12352211

• Target :

  Polo-like Kinase (PLK)

• Related Pathways :

  Cell Cycle/DNA Damage

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Purity :

  98.77

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  CC1=CC(NC2=NC(N(C3=C(C=C(C=C3F)S(C)(=O)=O)F)C)=NC(C4=CN(C=N4)C)=C2C5CC5)=NN1

• Molecular Formula :

  C23H24F2N8O2S

• Molecular Weight :

  514.55

• References & Citations :

  [1]Isabel Soria-Bretones, et al. A dual mechanism of sensitivity to PLK4 inhibition by RP-1664 in neuroblastoma. bioRxiv. February 17, 2025.|[2]Vallée F, et al. Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor. J Med Chem. 2025 Jun 12;68 (11) :10631-10647.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• Isoform :

  PLK4

• CAS Number :

  [2980682-00-4]