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