A MELK inhibitor
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MELK-8a (hydrochloride)

Item No. 37025

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-methyl-4-[4-[4-[3-(4-piperidinylmethoxy)-4-pyridinyl]-1H-pyrazol-1-yl]phenyl]-piperazine, monohydrochloride
CAS Number
2096992-20-8
Synonyms
  • NVS-MELK8a
Molecular Formula
C25H32N6O • HCl
Formula Weight
469.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: insolDMSO: insolEthanol: insolPBS (pH 7.2): 1 mg/ml
λmax
307 nm
SMILES
CN(CC1)CCN1C(C=C2)=CC=C2N3C=C(C(C=CN=C4)=C4OCC5CCNCC5)C=N3.Cl
InChi Code
InChI=1S/C25H32N6O.ClH/c1-29-12-14-30(15-13-29)22-2-4-23(5-3-22)31-18-21(16-28-31)24-8-11-27-17-25(24)32-19-20-6-9-26-10-7-20;/h2-5,8,11,16-18,20,26H,6-7,9-10,12-15,19H2,1H3;1H
InChi Key
AFGMSRRNYDSRPT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $108

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    10 mg

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    25 mg

    $351

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    50 mg

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    Product Description

    MELK-8a is an inhibitor of maternal embryonic leucine zipper kinase (MELK; IC50 = 0.002 µM).1 It is selective for MELK over FLT3, haspin, KIT, and PDGFRα, (IC50s = 0.18, 0.19, >10, and 0.42 µM, respectively), as well as a panel of 456 kinases at 1 µM. MELK-8a inhibits the proliferation of MDA-MB-468 and MCF-7 breast cancer cells (IC50s = 0.11 and 3.68 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Touré, B.B., Giraldes, J., Smith, T., et al. Toward the validation of maternal embryonic leucine zipper kinase: Discovery, optimization of highly potent and selective inhibitors, and preliminary biology insight. J. Med. Chem. 59(10), 4711-4723 (2016).