A Plk4 inhibitor
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RP 1664

Item No. 44283

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-cyclopropyl-N2-(2,6-difluoro-4-(methylsulfonyl)phenyl)-N2-methyl-6-(1-methyl-1H-imidazol-4-yl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
CAS Number
2980682-00-4
Molecular Formula
C23H24F2N8O2S
Formula Weight
514.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
CC1=CC(NC2=C(C3CC3)C(C4=CN(C)C=N4)=NC(N(C(C(F)=CC(S(C)(=O)=O)=C5)=C5F)C)=N2)=NN1
InChi Code
InChI=1S/C23H24F2N8O2S/c1-12-7-18(31-30-12)27-22-19(13-5-6-13)20(17-10-32(2)11-26-17)28-23(29-22)33(3)21-15(24)8-14(9-16(21)25)36(4,34)35/h7-11,13H,5-6H2,1-4H3,(H2,27,28,29,30,31)
InChi Key
POKVQQVLRJLUAK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $138

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    5 mg

    $654

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    10 mg

    $1,238

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    Product Description

    RP 1664 is an inhibitor of polo-like kinase 4 (Plk4; IC50 = 3 nM).1 It induces centriole depletion in hTERT RPE-1 retinal pigment cells (EC50 = 0.13 µM). RP 1664 induces cytotoxicity in MCF-7 breast cancer cells (EC50 = 0.051 µM). It reduces tumor volume in a CAL-148 breast cancer mouse xenograft model when administered at doses of 11 or 21 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vallée, F., Casás-Selves, M., Bubenik, M., et al. Discovery of RP-1664: A first-in-class orally bioavailable, selective PLK4 inhibitor. J. Med. Chem. 68(11), 10631-10647 (2025).