NVP-MELK8a hydrochloride

CAS No. 2096992-20-8

NVP-MELK8a hydrochloride( MELK8a hydrochloride )

Catalog No. M13303 CAS No. 2096992-20-8

NVP-MELK8a hydrochloride (MELK8a hydrochloride)?is a novel potent, and selective MELK inhibitor with IC50 of 2 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    NVP-MELK8a hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    NVP-MELK8a hydrochloride (MELK8a hydrochloride)?is a novel potent, and selective MELK inhibitor with IC50 of 2 nM.
  • Description
    NVP-MELK8a hydrochloride (MELK8a hydrochloride)?is a novel potent, and selective MELK inhibitor with IC50 of 2 nM; exhibits high selectivity with only 7 off-target kinases inhibited >85% against 456 kinases at 1 uM, Flt3 (IC50=0.18 uM), Haspin (IC50=0.19 uM), PDGFRα (IC50=0.42 uM); exhibits growth inhibition of MDA-MD-468 cells with IC50 of 0.11 uM, and increases cells harboring 4N DNA content.
  • In Vitro
    MELK-8a remains very potent (IC50=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2 μM, respectively.
  • In Vivo
    Subcutaneous administration of MELK-8a at 30 mg/kg in C57BL/6 mice results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (Tmax=0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, when administered orally at 10 mg/kg in C57BL/6 male mice, it shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance.
  • Synonyms
    MELK8a hydrochloride
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    MELK
  • Recptor
    MELK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2096992-20-8
  • Formula Weight
    469.02212
  • Molecular Formula
    C25H33ClN6O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 8.6 mg/mL (Need ultrasonic and warming)
  • SMILES
    CN1CCN(CC1)C2=CC=C(C=C2)N3C=C(C=N3)C4=C(C=NC=C4)OCC5CCNCC5.Cl
  • Chemical Name
    Piperazine, 1-methyl-4-[4-[4-[3-(4-piperidinylmethoxy)-4-pyridinyl]-1H-pyrazol-1-yl]phenyl]-,hydrochloride

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Touré BB, et al. J Med Chem. 2016 May 26;59(10):4711-23. 2. Huang HT, et al. Elife. 2017 Sep 19;6. pii: e26693.
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