RP-1664

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].

Product Specifications

CAS Number

[2980682-00-4]

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.