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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.
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. |
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. [1] |
Synonyms | RP1664 |
Molecular Weight | 514.55 |
Formula | C23H24F2N8O2S |
Cas No. | 2980682-00-4 |
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 |
Relative Density. | no data available |
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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (155.48 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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