RP-1664

SKU: orb3029071

Description

RP-1664 is a selective and orally active PLK4 inhibitor with an IC50 of 3 nM. This compound demonstrates exceptional selectivity over related kinases, disrupts centriole biogenesis in cancer cells leading to PLK4 and p21 protein accumulation, shows enhanced sensitivity in TRIM37-high-expressing cells, and exhibits antitumor activity in breast cancer and neuroblastoma research.

Research Area

Cell Biology

Key Properties

• CAS Number: 2980682-00-4
• MW: 514.55
• Purity: 99.04%
• Formula: C₂₃H₂₄F₂N₈O₂S
• SMILES: O=S(=O)(C1=CC(F)=C(C(F)=C1)N(C=2N=C(NC3=NNC(=C3)C)C(=C(N2)C=4N=CN(C4)C)C5CC5)C)C
• Target: PLK
• Solubility: DMSO:80 mg/mL (155.48 mM)

Bioactivity

• In Vitro:
  Methods: RPE1-hTERT Cas9 TP53 knockout cells and RPE1-hTERT Cas9 TP53 wild-type cells were treated with RP-1664 (1-1000 nM, 48-72 hours), and the expression of target proteins was analyzed by Western Blot. Results: The total protein level of PLK4 was increased in RPE1-hTERT Cas9 TP53 knockout cells, and the level of p21 protein was increased in RPE1-hTERT Cas9 TP53 wild-type cells in a dose-dependent manner.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RP1664

Quick Database Links

Gene Symbol

PLK