2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. 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].

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RP-1664 Chemical Structure

RP-1664 Chemical Structure

CAS No. : 2980682-00-4

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Based on 1 publication(s) in Google Scholar

RP-1664 Related Antibodies

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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].

IC50 & Target[1]

PLK4

 

In Vitro

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.

RP-1664 Related Antibodies

Western Blot Analysis[1]

Cell Line: RPE1-hTERT Cas9 TP53-null cells and RPE1-hTERT Cas9 TP53-WT cells
Concentration: 1-1000 nM
Incubation Time: 48-72 h
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.
In Vivo

RP-1664 (600 ppm, oral administration via feed, 7 days on/7 off or 14 days on/7 off or daily for 40 days) exhibits dose-dependent anti-tumor activity in MCF7 xenograft mice[1].
RP-1664 (300 ppm, oral administration via feed, 17 days on/7 off for 40 days) elicits robust anti-tumor activity in NBL models through low-dose-induced centrosome amplification[1].
RP-1664 (compound 37) (6-21 mg/kg, i.g., twice a day, 35 days) shows dose responsive tumor growth inhibition, stasis and regressions in CAL-148 xenograft mice[2].
RP-1664 (300-600 ppm, oral administration via feed, 3 days on/4 off or 14 days on/7 off or daily for 55 days) inhibits tumor growth in CHP-134 xenograft mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 600 ppm
Administration: p.o. on schedules of 7 days on/7 off or 14 days on/7 off or daily for 40 days
Result: Inhibited the tumor growth with maximal tumor growth inhibition (TGI) of 95% at 600 parts per million (ppm).
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]
Dosage: 300 ppm
Administration: p.o. on schedules of 17 days on/7 off for 40 days
Result: Suppressed tumor growth regardless of TRIM37 or TP53 inactivation.
Animal Model: Female SCID-beige mice xenografted with CAL-148 cells (5-7 weeks) (107 cells per mouse)[2]
Dosage: 6, 11, 21 mg/kg
Administration: i.g. for 35 days
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.
Animal Model: Female CB-17 SCID mice bearing subcutaneous CHP-134 xenografts (5-7 weeks) (107 cells per mouse)[2]
Dosage: 300, 600 ppm
Administration: p.o. on schedules of 3 days on/4 off or 14 days on/7 off or daily for 55 days
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.
Clinical Trial
Molecular Weight

514.55

Formula

C23H24F2N8O2S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9434 mL 9.7172 mL 19.4345 mL
5 mM 0.3887 mL 1.9434 mL 3.8869 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

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
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
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RP-1664 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RP-16642980682-00-4RP1664RP 1664Polo-like Kinase (PLK)PLK4MCF7CHP-134CAL-148cancercentrioleInhibitorinhibitorinhibit

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