A selective Plk1 inhibitor
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Ro 3280

Item No. 21669

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide
CAS Number
1062243-51-9
Molecular Formula
C27H35F2N7O3
Formula Weight
543.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLEthanol: 30 mg/mLEthanol:PBS(pH 7.2) (1:1): 0.5 mg/mL
λmax
287, 328 nm
SMILES
O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N(C)C(C(F)(F)CN4C5CCCC5)=O)C4=N3)C=C2
InChi Code
InChI=1S/C27H35F2N7O3/c1-34-12-10-18(11-13-34)31-24(37)17-8-9-20(22(14-17)39-3)32-26-30-15-21-23(33-26)36(19-6-4-5-7-19)16-27(28,29)25(38)35(21)2/h8-9,14-15,18-19H,4-7,10-13,16H2,1-3H3,(H,31,37)(H,30,32,33)
InChi Key
DJNZZLZKAXGMMC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $151

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    10 mg

    $280

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    25 mg

    $653

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    Product Description

    Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.1 Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.1,2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, S., Bartkovitz, D., Cai, J., et al. Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg. Med. Chem. Lett. 22(2), 1247-1250 (2012).

    2. Tao, Y.-F., Li, Z.-H., Du, W.-W., et al. Inhibiting PLK1 induces autophagy of acute myeloid leukemia cells via mammalian target of rapamycin pathway dephosphorylation. Oncol. Rep. 37(3), 1419-1429 (2017).

    3. Zhang, Z., Zhang, G., and Kong, C. Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells. J. Cell. Mol. Med. 21(4), 758-767 (2017).

    4. Wang, N.-N., Li, Z.-H., Zhao, H., et al. Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int. J. Mol. Sci. 16(1), 1266-1292 (2015).