RP-1664
Based on 1 Customer Validation
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].
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- Pureza: 98.77%
- No. CAS: 2980682-00-4
- Fòrmula: C23H24F2N8O2S
- Peso molecular:514.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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PLK4 |
RP-1664 (1-1000 nM, 48-72 h) increases total PLK4 protein levels in RPE1-hTERT Cas9 TP53-null cells and increases p21 protein levels in RPE1-hTERT Cas9 TP53-WT cells dose dependently[1]. RP-1664 (0.001-10 μM) demonstrates a ~30-fold increase in sensitivity between TRIM37-normal/TP53-KO cells and TRIM37-overexpressing/TP53-WT cells, with intermediate sensitivity observed in TRIM37-high/TP53-KO and TRIM37-normal/TP53-WT cells[1]. RP-1664 (50-250 nM) induces centrosome loss at concentrations >100 nM in both p53-proficient and -deficient RPE1 cells as well as in three different NBL cell lines (CHP134, CHP212, SHSY5Y)[1]. RP-1664 (50-250 nM) induces supernumerary centrosomes between 25-100 nM in both p53-proficient and -deficient RPE1 cells[1]. RP-1664 (0-2000 nM, 48 h) enhances cellular sensitivity to PLK4 inhibition and centrosome depletion in a manner dependent on high TRIM37 protein levels and functional p53[1]. RP-1664 (compound 37) shows an EC50 of 0.051 μM in reducing MCF7 cell viability[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RPE1-hTERT Cas9 TP53-null cells and RPE1-hTERT Cas9 TP53-WT cells
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Concentration:1-1000 nM
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Incubation Time:48-72 h
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Result:Increased total PLK4 protein levels in RPE1-hTERT Cas9 TP53-null cells.
Increased p21 protein levels in RPE1-hTERT Cas9 TP53-WT cells dose dependently.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c Nude mice were supplemented with estradiol in drinking water (2.5 µg/mL) and gamma irradiated (1.2 Gy) 1 week and 24-72 hours prior to inoculation in the right flank using 10 million MCF7 cells[1]
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Dosage:600 ppm
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Administration:p.o. on schedules of 7 days on/7 off or 14 days on/7 off or daily for 40 days
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Result:Inhibited the tumor growth with maximal tumor growth inhibition (TGI) of 95% at 600 parts per million (ppm).
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Animal Model:Female CB/17 SCID mice were inoculated in the right flank with 10 million cells of either parental CHP134, CHP134 TP53-KO or CHP134 TRIM37-KO[1]
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Dosage:300 ppm
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Administration:p.o. on schedules of 17 days on/7 off for 40 days
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Result:Suppressed tumor growth regardless of TRIM37 or TP53 inactivation.
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Animal Model:Female SCID-beige mice xenografted with CAL-148 cells (5-7 weeks) (107 cells per mouse)[2]
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Dosage:6, 11, 21 mg/kg
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Administration:i.g. for 35 days
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Result:Showed tumor growth inhibition at 6 mg/kg.
Showed tumor growth stasis at 11 mg/kg.
Showed tumor growth regressions at 21 mg/kg.
Increased protein levels of PLK4 or p21 for 4 to 11 days.
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Animal Model:Female CB-17 SCID mice bearing subcutaneous CHP-134 xenografts (5-7 weeks) (107 cells per mouse)[2]
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Dosage:300, 600 ppm
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Administration:p.o. on schedules of 3 days on/4 off or 14 days on/7 off or daily for 55 days
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Result:Improved the tumor regressions efficacy with longer continuous exposure.
Improved tolerability with intermittent dosing, whereas continuous dosing at 600 ppm was not tolerated beyond day 46.
Increased protein levels of PLK4 or p21 for 4 to 11 days.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2980682-00-4
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Appearance Solid
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Peso molecular 514.55
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Fòrmula C23H24F2N8O2S
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (194.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9434 mL | 9.7172 mL | 19.4345 mL | 48.5861 mL |
| 5 mM | 0.3887 mL | 1.9434 mL | 3.8869 mL | 9.7172 mL | |
| 10 mM | 0.1943 mL | 0.9717 mL | 1.9434 mL | 4.8586 mL | |
| 15 mM | 0.1296 mL | 0.6478 mL | 1.2956 mL | 3.2391 mL | |
| 20 mM | 0.0972 mL | 0.4859 mL | 0.9717 mL | 2.4293 mL | |
| 25 mM | 0.0777 mL | 0.3887 mL | 0.7774 mL | 1.9434 mL | |
| 30 mM | 0.0648 mL | 0.3239 mL | 0.6478 mL | 1.6195 mL | |
| 40 mM | 0.0486 mL | 0.2429 mL | 0.4859 mL | 1.2147 mL | |
| 50 mM | 0.0389 mL | 0.1943 mL | 0.3887 mL | 0.9717 mL | |
| 60 mM | 0.0324 mL | 0.1620 mL | 0.3239 mL | 0.8098 mL | |
| 80 mM | 0.0243 mL | 0.1215 mL | 0.2429 mL | 0.6073 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4859 mL |
RP-1664 Related Classifications
HY-172737 Related Classifications
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