A polo-like kinase inhibitor
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BI-6727

Item No. 18193

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide
CAS Number
755038-65-4
Synonyms
  • Volasertib
Molecular Formula
C34H50N8O3
Formula Weight
618.8
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
330 nm
SMILES
CC[C@@H]1C(N(C)C2=CN=C(NC3=C(OC)C=C(C(N[C@@H]4CC[C@@H](N5CCN(CC6CC6)CC5)CC4)=O)C=C3)N=C2N1C(C)C)=O
InChi Code
InChI=1S/C34H50N8O3/c1-6-28-33(44)39(4)29-20-35-34(38-31(29)42(28)22(2)3)37-27-14-9-24(19-30(27)45-5)32(43)36-25-10-12-26(13-11-25)41-17-15-40(16-18-41)21-23-7-8-23/h9,14,19-20,22-23,25-26,28H,6-8,10-13,15-18,21H2,1-5H3,(H,36,43)(H,35,37,38)/t25-,26-
InChi Key
SXNJFOWDRLKDSF-STROYTFGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $157

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    10 mg

    $274

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    25 mg

    $583

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    Product Description

    Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.1 BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.2 It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.2 BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schöffski, P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist 14(6), 559-570 (2009).

    2. Rudolph, D., Steegmaier, M., Hoffmann, M., et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin. Cancer Res. 15(9), 3094-3102 (2009).

    3. To, K.K.W., Poon, D.C., Chen, X.G., et al. Volasertib (BI 6727), a novel polo-like kinase inhibitor reverses ABCB1 and ABCG2-mediated multidrug resistance in cancer cells. J.Cancer Ther.Res. 2(13), 1-10 (2015).