An inhibitor of Plk1
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NMS-1286937

Item No. 28762

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,5-dihydro-1-(2-hydroxyethyl)-8-[[5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
CAS Number
1034616-18-6
Synonyms
  • NMS-P937
  • Onvansertib
  • PCM-075
Molecular Formula
C24H27F3N8O3
Formula Weight
532.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5mg/mLDMF:PBS (pH 7.2) (1:3): 0.25mg/mLDMSO: 3mg/mL
SMILES
CN1CCN(C2=CC=C(OC(F)(F)F)C(NC3=NC=C(CCC4=C5N(CCO)N=C4C(N)=O)C5=N3)=C2)CC1
InChi Code
InChI=1S/C24H27F3N8O3/c1-33-6-8-34(9-7-33)15-3-5-18(38-24(25,26)27)17(12-15)30-23-29-13-14-2-4-16-20(22(28)37)32-35(10-11-36)21(16)19(14)31-23/h3,5,12-13,36H,2,4,6-11H2,1H3,(H2,28,37)(H,29,30,31)
InChi Key
QHLVBNKYJGBCQJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    NMS-1286937 is an inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM).1 It is selective for Plk1 over Plk2 and Plk3 (IC50s = >10,000 nM for both). It inhibits proliferation of A2780 cells with an IC50 value of 42 nM. NMS-1286937 halts the cell cycle at the G2/M phase in A2780 cells when used at a concentrations ranging from 20 to 200 nmol/L and induces apoptosis.2 It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 60 mg/kg once per day.1 NMS-1286937 (45 mg/kg) also induces tumor regression in an HT-29 mouse xenograft model when administered in combination with CPT11 (irinotecan; Item No. 14180).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beria, I., Bossi, R.T., Brasca, M.G., et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg. Med. Chem. Lett. 21(10), 2969-2974 (2011).

    2. Valsasina, B., Beria, I., Alli, C., et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol. Cancer Ther. 11(4), 1006-1016 (2012).