A potent inhibitor of Plk1
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BI-2536

Item No. 17385

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide
CAS Number
755038-02-9
Molecular Formula
C28H39N7O3
Formula Weight
521.7
Purity
≥95%
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
210, 249, 345 nm
SMILES
O=C1[C@@H](CC)N(C2CCCC2)C3=NC(NC4=C(OC)C=C(C(NC5CCN(C)CC5)=O)C=C4)=NC=C3N1C
InChi Code
InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
InChi Key
XQVVPGYIWAGRNI-JOCHJYFZSA-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

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    10 mg

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    50 mg

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    Product Description

    BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).1,2 It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.1 It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.3 BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Steegmaier, M., Hoffmann, M., Baum, A., et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Curr. Biol. 17(4), 316-322 (2007).

    2. Peifer, C., and Alessi, D.R. Small-molecule inhibitors of PDK1. ChemMedChem 3(12), 1810-1838 (2008).

    3. Danovi, D., Folarin, A., Gogolok, S., et al. A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1. PLoS One 8(10), 1-13 (2013).

    4. Ciceri, P., Müller, S., O'Mahony, A., et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat. Chem. Biol. 10(4), 305-312 (2014).